TW200427680A - N-(substituted arylmethyl)-4-(disubstituted methyl)piperidines and pyridines - Google Patents

Abstract

It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): , wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Description

200427680 (ii) Description of the invention: [Technical field to which the invention belongs] The present invention generally relates to insecticidal compounds and their uses for controlling insects. In particular, the present invention relates to insecticidal N- (substituted aryl), 4- (disubstituted methyl) hexahydropyridine and pyridine derivatives, N-oxides and agriculturally acceptable salts thereof. Classes, compositions of these insecticides and their methods for controlling insects. [Prior art] It is well known that insects can often cause significant damage. 'The damage caused by native insects (such as Bai Yi and Pesticide) is not only related to crops grown in agriculture, but also to structures and grasslands. These damages can cause millions of dollars worth of damage associated with established crops' grasslands or structures, and there is a continuing need for new, more effective and lower cost new insecticides. Insecticides are used to control insects that can cause significant damage to a small number of named crops (A, W, Yuwei, Daiwa, Potato, and Cotton) in different ways. Right: ^ Harmful crops can control insects and killing mammals and their living organisms without adverse effects. Many patents disclose a variety of crops with killing properties. Hexahydropyridine derivatives. For example, ra <the substituted hexahydropyridine and its proposed compound having insecticidal activity as described in Patent No. 5,569,664 'and a compound having the following structure:

QY 90038 200427680 where U is selected from-(CHI * ethylidene (Changchong where ^ system is' 2 or 3), Q is selected from hydrogen, hydroxyl, hydrogenthio and fluorine; v is selected from hydrogen, Halogen, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsilyloxy, dialkylamino, cyano, nitro, hydroxyl, and phenyl; w is selected From hydrogen, quotient, alkyl, alkyl, alkoxy, nitro, amine, phenoxy and phenylalkoxy, X is selected from hydrogen, hydroxyl, halogen, alkyl, alkoxy Alkyl, alkoxy, cycloalkylalkoxy, alkoxy, alkenyl, alkynyl, alkynyl, sulfenyl, thio, thio, thio, cyano, cyano Base, alkynyl, amine, monoalkylamino, dialkylamino, alkylaminoalkoxy, pentylamino, alkoxycarbonylamino, alkylcarbonyl, alkoxycarbonyl, alkylamino Group, aminocarbonyloxy, phenyl, phenylalkoxy, phenoxy, and phenoxyalkyl; Y and Z are independently selected from hydrogen and alkyl; R1 and R2 are independently selected from , Alkyl, haloalkyl, alkoxy, alkoxyalkyl, hydroxyl, arylthio , Alkoxy, dialkylamino, dialkylaminosulfonyl, hydroxyalkylaminocarbonyl, alkylsulfonyloxy, and alkanesulfonyloxy substituted phenyl groups; and corresponding N-oxidation And agriculturally acceptable salts. As described in US Patent No. 5,639,763, it proposes compounds having the following structure with insecticidal activity:

Where U is selected from-(CH2) n- and ethylidene (where η is 1, 2 or 3), Q is selected from hydrogen, hydroxyl, hydrogenthio, and fluorine; V is selected from hydrogen, halo, and alkyl Alkyl, halo 90038 -10- 200427680 alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylmethyloxy, dialkylamino, cyano, nitro, hydroxyl, and phenyl; ¥ and z are independently selected from the group consisting of hydrogen and a few alkoxy groups, and W and X together are -OCH ^ CH ^ O-, -〇C (CH3) 20-, or -N = C (C2H5) 〇-; R1 and R2 Is independently selected from the group consisting of alkyl, alkyl, haloalkyl, haloalkoxy, alkoxyalkyl, hydroxy, arylthio, anti-lactyl, monoamine, diamine, and Alkylamino, sulfanyl, and alkylsulfonyloxy substituted phenyl groups; and corresponding N_ oxides and agriculturally acceptable salts.

As described in U.S. Patent No. 5,795,901, it proposes compounds having the following structure with insecticidal activity:

[Anion] wherein V, W, γ and Z are hydrogen; X is alkoxy, cycloalkoxy, alkoxycarbonyl, alkoxycarbonylamino or 5- or 6-membered heteroaryl or heteroaryloxy Group, each heteroaryl group is optionally substituted with halogen, cyano, alkyl, fluorenyl, alkoxy, haloalkoxy or haloalkoxyalkyl; R1 and R2 are independently selected from haloalkyl Phenyl substituted with halo, self-thio, haloalkyl, or haloalkoxy; or 5- or 6-membered heteroaryl substituted with halogen or alkyl; R3 is alkyl, haloalkyl, hydroxy Alkyl, alkoxyalkyl, dialkylaminoalkyl, alkylaminocarbonyloxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, alkylcarbonyloxyalkyl, alkoxy Carboxyalkyl, carboxyalkyl, carboxyarylalkyl, arylcarbonyl, sulfonate or sulfonate 90038 -11-200427680 alkyl, and can carry a negative charge to form internal salts, as well as separate anion lice and bromide , Iodide, or sulphuric acid or phenyl or sulfonate, as described in US Patent No. 5,939,438, which proposes compounds having the following structure with insecticidal activity:

Wherein R is hydrogen, halogen, alkyl, alkoxy or dialkylamino; Rl is hydrogen, alkyl, IS, alkoxyalkyl, alkylcarbonyl or alkylaminocarbonyl; q is fluoro or X-based oxygen or NR2; Z-based halogen, haloalkyl, haloalkoxy, pentahalothio, pinanethio, _alkylthiosulfenyl, alkylsulfonyl or attached to phenyl When two adjacent carbon atoms of the ring are 0 (^ 2〇-; ^ system; and when X is NR2, then R2 is hydrogen, alkyl, alkylcarbonyl, alkoxycarbonyl, or R and R2 together Can be (of which 111 is 3-9); and agriculturally acceptable salts thereof. As described in US Patent No. 6,017,931, it proposes compounds having the following structure with insecticidal activity:

V, W and Z are hydrogen; X is selected from alkoxy, haloalkoxy, and alkoxy 90038 -12- 200427680

Radical, alkoxy, alkoxy, alkoxy, alkoxy, alkoxy I, halo: alkoxy, alkoxy, alkoxy, alkoxy Alkyl, alkoxyalkoxycarbonyl, alkoxycarbonylamino, alkoxycarbonylamino, cycloalkylthioalkyl, cycloalkylamino, alkylamino, alkylamine Radical, #alkylaminocarbonyl, cyanoalkoxyamino, phenylcarbonylamino and phenoxycarbonyl, each cycloalkyl moiety or phenyl ring is substituted with halogen as needed; Y is selected from Hydrogen or halogen; R1 and R2 are independently selected from phenyl or pyridyl, each of which is substituted with _alkyl, haloalkoxy or alkylthio; and corresponding N-oxides and agriculturally acceptable salts class. As described in U.S. Patent No. 6,030,987, it proposes compounds having the following structure with insecticidal activity:

Among them, V, W, γ and z are hydrogen; X is optionally halogen, alkyl, alkoxy, pitoxy, feno, cyano, aminozoyl, endyl, halooxy or halooxy. 5- or 6-membered heterocyclic ring substituted with alkyl group; and the heterocyclic ring is optionally connected to the phenyl ring via -0,-,-(CH2) r, -c (〇)-, or R1 and R2 are independent Selected from phenyl or pyridyl, each of which is substituted with haloalkyl or halooxy; R3 and R4 are independently selected from hydrogen and methyl; η and p are independently 1, 2, or 3; and q is 1 Or 2, and the corresponding N-oxides and agriculturally acceptable salts. As described in U.S. Patent No. 6,184,234, it proposes compounds having the following structures having insecticidal activity 90038 -13-200427680:

/ 、 Medium V w ¥ and 2 series hydrogen; X series if necessary, bromine, chlorine, fluorine, tiger group, alkoxy group = oxyalkyl group, cyano group, aminocarbonyl group, fluorenyl group, _oxy group or iS k A 5- or 6-membered heterocyclic ring substituted with an oxyk group; and the heterocyclic ring is optionally connected to a phenyl ring via 0 S (CIi2V, -c (〇)-or -0 (CR3R4) q-, R and R are independently selected from i) phenyl or pyridyl, each of which is substituted with pentahalothio, is alkylthio, sulphanylsulfenyl, or from alkylsulfonyl, Π) with-. C (M) 20-substituted phenyl, where M is bromine, chlorine, or fluorine, providing a dihalobenzo-oxapentyl fused ring; or iii) replacing the other dangling group 'to provide two Halodioxolene · cyclopyridyl fused rings; R3 and R4 are independently JL selected from hydrogen and methyl; n and P are independently 1, 2, or 3; and q is 1 or 2, and the corresponding N -Oxides and agriculturally acceptable salts. As described in U.S. Statutory Invention Registration H1,838, it proposes compounds having the following structure with insecticidal activity:

Where m is 2 or 3; η is 0 or 1; X is hydrogen, alkoxy, cycloalkylalkoxy 90038 -14-200427680, from alkoxyimino or 5- or 6-membered heteroaryl Or will be — soil &amp; glutamate, in which a heteroatom may be substituted with an alkyl group as needed; r ^ r2 is independently selected from two: Nanxian, sulfanyl or fluorenyl; and when ... Y represents ⑷ • minus; or ⑻ ring nitrogen is an agriculturally acceptable anionic salt; 2 (c) forming an OR3 bond, wherein R3 is selected from the group consisting of chloro 4 4 砭 砭, alkoxycarbonyl 叛 叛 乙 乙 ethyl And an agriculturally acceptable anion group that forms an ionic salt, or R3 is an oxycarbonyl group that carries a negative t charge that forms an internal salt. , As described in U.S. Statutory Invention Registration H1,996, which proposes an insecticidal activity

R1 f. Photochemically stable agriculturally acceptable acid salts of organic or inorganic acids of the following structures: where R is: alkoxyl, alkynylamino, cycloalkynyl , 2-alkyl-2H-tetrazol-5-yl or 2-haloalkyl-2H-tetrazol-5-yl; R1 is trisalkenyl or trisoxy, η is 0 or 1; and This salt has 2.5 to 5 times higher light stability than its non-ionic parent, and is derived from hydrogen acid, hydrobromic acid, boric acid, phosphoric acid, maleic acid, fumaric acid, phthalic acid, D-glucuronic acid , Sulfonic acid R2S〇3H (where R2 is alkyl, haloalkyl, hydroxylamine, D-10-camphoryl or phenyl substituted with alkyl or halogen if necessary), carboxylic acid R3CO2H (where R3 is hydrogen , Alkyl, trisynyl, &amp; base, optionally substituted with pit group or 1¾ element, peptidyl group and p-pyridyl group), surface acid R4B (〇H) 2 (where R4 is alkyl group or as needed Alkyl or halogen is 90038 -15-200427680 phenyl) Phosphonic acid R5po3H2 (where r5 is alkyl, fluorenyl or phenyl substituted with alkyl or halogen if necessary), R6SOS sulfate. 3H (where R6 is a &lt; ^ group) or alkanoic acid X-CCHdqCC ^ H (where q is 0 To! I, actinide, dinanyl, haloyl, amino, amino, or CO2R /, of which R7 is gas and aryl. As described in U.S. Legal Invention Registration H2,007, it proposes compounds having the following structure with insecticidal activity:

Wherein A and B are independently selected from lower alkyl groups; u is selected from low carbon alkyl, low carbon and CH-Z (where Z is selected from hydrogen, low carbon alkyl, low carbon cycloalkyl or benzene Group); R-CHR3R4 'where ^ and 4 are independently selected from the group consisting of 2 primes, lower alkyls, lower alkyls, lower alkyls, lower alkyls, and lower alkyls Phenyl or phenyl substituted phenyl; R1 is phenyl, naphthyl, tetratylphenyl, phenylcyclopropyl, phenoxyphenyl, benzyloxyphenyl, pyridylphenyl, and pyridine Basic group or ρ plugs a monooxyphenyl group, and each one will be a commercial group, a cyano group, a hydroxy group, a lower alkyl group, a lower alkyl group, a lower alkyl group, an amino group, and a lower alkyl group as needed. Amino, Nitro, Low-Carbon || Alkylsulfonyloxy, Low-Carbon * Hydroxy, Low-Carbon Alkylamino, Low-Carbon Alkoxycarbonyl, Low-Carbon Alkoxy, Carboxyl, Low Carbocycloalkylalkoxycarbonyl, lower alkoxyalkoxycarbonyl, lower alkoxycarbonylamino, alkoxythiocarbonylamino, lower carbon dithiocarbonylamino, lower carbon dialkyl Dioxopentenylalkoxycarbonyl Substituted, or a lower alkyl group substituted with any one of the above-mentioned ring systems r1 90038 -16- 200427680; η system 2 or 3; and η system 1, 2 or 3. As described in the unexamined Japanese patent application 2002-220372, it proposes compounds having the following structure having insecticidal activity:

Wherein R1 and R2 are independently selected from hydrogen, halogen, lower alkyl, lower alkyl, lower alkyl, lower alkyl, lower alkyl, or lower alkyl sulfonyl; , Lower alkyl, lower alkenyl, lower alkoxyalkyl or lower alkoxycarbonyl; X and Υ are independently oxygen or sulfur; R3 is selected from lower alkenyl or lower alkynyl If necessary, the hydroxyl group, halogen, low-carbon alkoxy group, low-carbon haloalkoxy group, low-carbon thio group, low-carbon sulfite group, low-carbon alkanoate group, low-carbon ring group, Lower alkoxy alkoxy, amine, lower alkamino, lower carbodialkyl, lower alkoxy, nitro, cyano, trimethylsilyl, phenyl or Lower carbocyclic alkenyl substitution; and corresponding N-oxides and salts. As described in the PCT publication, 0 02/068392 A1, it proposes compounds having the following structure with insecticidal activity:

90038 200427680 where R and R are independently selected from halogen, radical, halo Ci-C6: J ^ group, c "c6 alkoxy, halooxy ... S (= 0) p-R9 or S] p5; R3 Based on hydrogen, hydroxyl, CVC ^ oxy or -OCPCO-CVQ alkyl, R4 based on hydrogen, carbon, CVC6 alkyl, halo Cl_c6 alkyl, C! -C6 alkyloxy, halo cvc6 alkoxy or -S (= 0) p-R9 or _SCN; R5 & r6 is independently selected from c! _Ci2 alkyl, IS group cvc12 alkyl, C2-Cl2 alkenyl, fluorenyl c2_Ci2 alkenyl, 〇2 meaning 2 alkynyl , I-group c2-c12 alkynyl, (: 3-(: 8cycloalkyl, -c (= 〇) -〇r7, -C BS) -〇r8, -C (= Y) -ZR8 ... s ( = 〇Vr9, aryl, arylalkyl, heterocyclic, heterocyclic ct-C6 alkyl, each of which is independent of each other in the ring with halogen, vanyl, cyano, nitro, CVC6 alkyl, halo Cl_c6 Alkyl, alkyl, halo CrC6 alkoxy substitutions from 1 to 5 times; or together with their attached &lt; nitrogen atom to form a substituted or unsubstituted heterocyclic ring; Y is oxygen or sulfur ; X series bond, -NR1 or sulfur; R7 series Ci_C6 alkoxy- (Vc6 alkyl, dagger- (: 6 alkylthio-CVC6 alkyl, Cl_c6 amine-Ci_c6 alkyl, alkynyl, Cl-C6 Fluorenyl-S (== 〇VCi -C6 alkyl, CrC8 cycloalkyl, aryl, square-CrC6 alkyl, heterocyclyl, or heterocyclyl alkyl, each of which is independently of one another in the ring by M, cyano, nitro, C, C6 The alkyl group and the alkynyl group are substituted by 6 alkyl groups, C, c6 alkyloxy groups, or substituted by the group Ci {6 alkyloxy groups; R8 is a Cl_C6 alkyl group, a dentyl group, an alkyl group, and an alkyl group. , Cvc6sulfanyl-Cl-C6fluorenyl, C2_C6alkenyl, CrC6decyl, c ... carbonyl I-0) P-Cl collar, kc8 cyclopoyl, aryl, arylkc6 alkyl, heterocyclic Or heterocyclyl-ce to form a radical, or a cycloalkyl, aryl, aryl-CVC radical, heterocyclyl or heterocyclyl_C6 alkyl, each of which is independent of each other in the ring Element, cyano group, stone group, C-terminal group, self-group Cl-c6 90038 -18- 200427680 fluorenyl, C ^ c: 6 methoxy or halo CVC6 alkoxy substitution from 1 to 5 times; R9 is C ! -C6fe group, c3-C8 ring pit group, haloalkyl group or fluorenyl group; R10 is hydrogen, C6C6 alkyl, C3-C8 cycloalkyl, halo Cl_c6 alkyl or fluorenyl; p is 0, 1 or 2; q is 0 or 1; and if appropriate e / z isomers, E / Z isomer mixtures and / or tautomers, each of which is a free form or a salt form As the case of WO 2000 20409A1 PCT publication, which proposes compounds having insecticidal activity of the following structure:

Among them, R1 is a dental group, C1-C4 alkyl, C1-C4 alkyl, C1-C4 halo, C "C4 haloalkoxy; R2 is hydrogen, hydroxyl, halo, CVC4 alkyl, CVC4 alkoxy Group, Ci-G alkoxycarbonyl group, Crc4 alkylthio group, C! -C4 alkylsulfonyl group, optionally substituted phenyl or carbamoyl group; z is 0 or s (〇) P 'P system 0 or 2; and m and η are 0 or 1. As described in PCT publication WO 03 / 022808A1, it proposes compounds having the following structure having insecticidal activity:

90038 -19- 200427680 where R1 represents an aryl or heteroaryl group, and it is optionally substituted one or more times with the same or different times; R2 and R3 are the same or different, and represent a heteroaryl group, which is subject to a Or several times the same or different substitutions, so two groups can also be bridged with a common substituent; M is optionally substituted (CH2) i (where 1 is 1, 2, or 3), C0 or -HN -C (〇); X represents Η, OH, halogen, OR4 or CN; Y represents (〇), Η, OH, OR4, R4; (in the last 4 groups, wherein nitrogen has a Positive charge); R4 is the same or different, and represents ((VC4) alkyl, (CVCU) alkylfluorenyl, (CVC4) haloalkyl; m is 0, 1, 2, 3; and n is 0 or 1. As described in published Japanese patent application JP 62,145,018, it discloses the following compounds as anti-allergic pharmaceutical agents:

The hexahydropyridine or rhodamine derivatives of the present invention are not disclosed or suggested in any of the citations mentioned above. [Summary of the Invention] According to the present invention, it has now been found that when a specific N- (substituted arylmethyl) -4- (disubstituted methyl) hexahydropyridine and When pyridine derivatives (hereinafter referred to as, compounds of formula I), N-oxides and their agriculturally acceptable salts, they have unexpected activity. The compound of formula I is represented by the following general formula I: 90038 -20- 200427680

Where: m, η, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is selected from C and CH to form a group selected from hexahydropyridine, 1,4-di Hydropyridine and 1,2,5,6-tetrahydropyridine 6-membered acryl ring; R2, R3, R4, R5, and R6 are independently selected from hydrogen, halogen, alkyl, and halogen 'J: end, super Group, alkoxy, haloalkoxy, pentahalothio, alkylthio, cyano, nitro, alkylcarbonyl, alkoxycarbonyl, aryl or aryloxy, the prerequisites are at least one of R2, R3, R4, R5, and R6 are not hydrogen; and either R2 and R3, or R3 and R4, and -〇CF2〇-, -OCF2CF2-, -CF2CF2〇, or -CH = CHCH = CH --- form benzene And a fused ring; and (a) when m and η are 0; then a double bond is formed between the methyl carbon (a) and the 4-position of the 6-membered acryl well ring,

90038 -21-200427680 where B is R9, R1. , R11, R12 and R13 substituted phenyl,

R9, R10, R11, R12, and R13 are independently selected from the group consisting of hydrogen, halogen, alkyl, halogen, J: charge, trisoxy, alkyl, haloxy, sulfhydryl and thiothio, cyano, Alkylcarbonyl, alkoxycarbonyl or aryloxy; and either R9 and R1G, or R10 and R11 together with -〇CF20-, -OCF2CF2- or -CF2CF2〇- to form a benzo-fused ring, the prerequisites are: At least one of R9, R1 (), R11, R12, and R13 is not hydrogen; and (b) m-series 1 and η-series 0; then at the 4-position of the methyl carbon (a) and the 6-membered acryl ring Double bonds are formed,

Where B is a bridging group from methyl (a) to R; 90038 -22-200427680 where B is selected from 〇, S, * CH2〇, * OCH2, 〇C (= 〇) 〇, * OC (= 〇) NR15, * NR15C (= 〇) 〇, * 〇C (= S) NR15, * NR15C (= S) 0, * 〇CH2C (= 0) NR15, * NR15C (= 〇) CH2〇, * CH2〇C ( = 〇) NR15, * NR15C (= 0) 〇CH2, * NR15CH2, * CH2NR15, * NR15C (= 〇), * C (= 0) NR15, * NR15S〇2, * S〇2NR15, * NR15NHS〇2, * S〇2NHNR15, * 0C (= 0) NR15S02, * S〇2NR15C (= 〇) 〇, * 0C (= 0) NR15 CHR16, * CHR16NR15C (= 〇) 〇, * NR15C (= 〇) NR16, 1, 4-dioxocyclohexyl or 4-oxyhexahydropyridin-1-yl, where the asterisk represents the point of attachment to methyl ash (a); where R15 and R16 are independently selected from hydrogen, alkyl, and alkylaminocarbonyl And arylcarbonyl, where the aryl is optionally substituted with halogen, alkyl, alkoxy, iS, alkoxy, or nitro; where R is an alkyl, cycloalkyl, fluorenyl, or:]: End Oxyalkyl, or R is phenyl substituted with R17, Ri8, R19, R2G and R21;

Or R is bipyridyl-2-yl substituted by R18, R19, R20 and R21; 90038 -23-200427680

Or orbipyridin-3-yl substituted with R17, R19, R20 and R21;

Or pyridin-4-yl substituted with R17, R18, R20 and R21; R17

R20 or pyridin-3-yl substituted with R19, R2Q and R21;

R 19 R wherein R17, R18, R19, R2G and R21 are independently selected from hydrogen, halogen, alkyl, haloalkane 90038 -24-200427680, alkoxy, i-alkoxy, alkylthio, haloalkylthio , Cyano, nitro, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylamino, aryl, aryloxy, and 2-alkyl-2H-tetrazole, and one of them is taken as Ri7 &amp; Ri8, or R18 And R can form a benzo-fused ring with -CH2CH = CHCH2-, -〇CF2〇-, -〇CF2CF2-, or -CF2CFzO-; and (c) m and η are 1; then at methyl carbon (A) forms a single bond with the 4-position of the 6-membered acryl ring,

Wherein B is a bridging group from methyl carbon (a) to R; where B is selected from 〇, S, * CH2〇, * 〇CH2, 〇 (= 0) 〇, * 〇C (= 〇) NR15, * NRi5C (= 〇) 0, * 〇C (= S) NRi5, * NRi5C (= S) 0, * och2c (= 〇) NR15, * NR15C (= 0) CH2〇, * CH2OC (= 〇) NR15, * NR15C (= 〇) 〇CH2, * NR15CH2, * CH2NR15, * NR15C (= 〇), * C (= 〇) NR15, * NRi5S02, * S02NRi5, * NR15NHS02, * S〇2NHNR15, * OC (= 〇) NR 丨 5S02, * S〇2NR15C (= 0) 0, * OC (= 〇) NR15 CHR16, * CHR16NR15C (= 〇) 0, * NR15C (= 〇) NR16, 1,4-two 90038 -25- 200427680 oxygen Cyclohexyl or 4-oxyhexahydroanthyl-boxy, where the asterisk represents the point of attachment to methyl carbon (a); where Ri5 and Ri6 are as described above; and &amp; pit, cycloalkyl, alkenyl Or alkoxycarbonyl; or R is phenyl substituted with, Ri8, R19, R2G, and R21; pyridin-2-yl substituted with R18, R19, R20, and R21; mouth substituted with R17, R19, R20, and R21 Pyridin · 3-yl; pyridyl substituted with R17 ,, r2Q, and r21; or pyridyl substituted with R19, R20, and R21; where R17, R18, r19, R2G, and R21 are described as ;

R1 is selected from hydrogen, alkyl, alkoxyalkyl or aryl; when δp is 1, 2 or 3; then D is -CHy, and forms an azabicyclic derivative of 6-membered acryl ring; when When q is 0 and r is 1, an N-oxide derivative of a 6-membered acyclic ring nitrogen is formed; when q is 1 and r is 0 or 1, R is selected from alkyl, self-alkyl, and hydroxyl Alkyl, alkoxyalkyl, dialkylamino, alkoxy, thio, thio, thio, thio, thio Oxyalkyl, benzyl, aryl, aryl, arylcarbonyl, sulfonate or sulfonate alkyl groups, and can carry negative charges to form internal salts; and separate ionic chlorides, bromides, iodides, Or sulfuric acid or alkyl sulfonate or phenyl ester; when s is 0 or 1; R8 is selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkoxy, alkoxyalkyl, amine , Morpholinyl, optionally substituted indolyl, hexachloro 90038 -26- 200427680 pyridyl, optionally substituted (say pyridyl) alkenyl, optionally substituted 1,2,3,4- Tetrahydrofluorenyl, optionally substituted arylpyrazolyl, benzo [b] Phenyl, 5-hydropyrido [1,2a] pyrimidinone, optionally substituted 4-hydro-1,3-oxazolinolin [3,2a] pyrimidinone, 1,2,3,4 -Tetrahydroquinolinyl, 2-thio-1,3-dihydroquinazolinone, 1,3-dihydroquinazolinone, or benzo [c] azepinedione, in which The required substituent is selected from halogen, alkyl, oxy and nitro; or R8 is phenyl substituted with R22, R23, R24, R25 and R26,

R, RZ4, RU and substituted pyridin-2-yl;

Pyridin-3-yl substituted with R24, RU and R20;

90038 -27-200427680 or pyridin-4-yl substituted with R22, R23 'R25 and R26;

among them

R22, R23, R24, R25 and R26 are independently selected from hydrogen, halogen, alkyl, hydroxyl, alkoxy, alkoxyalkyl, dialkoxyalkyl, trialkoxyalkyl, alkoxy Aminoalkyl, alkenoxyiminoalkyl, alkynoxyiminoalkyl, cycloalkylalkoxy, alkoxyalkoxy, alkylthio, dithioalkoxyfe, tris Sulfuryloxy, alkynyl, acid, amine, ammonium, dialkylaminosulfonyl, cycloalkylaminosulfonyl, alkenyl, alkynyloxy, dilutedoxy, Basic alkoxy group, substituted aryl group as needed _ courtyard oxy group, cyano group, nitro group, amine group, amine group, carbamino group, carbamino group, alkoxy group Amine, decylamino, aminoalkylcarbonylamino, alkoxyalkoxycarbonylamino, (alkyl) (alkoxycarbonyl) amino, alkylsulfonylamino, Requires substituted (heteroaryl) (alkoxycarbonyl) amino group, optionally substituted arylcarbonylamino group, formamyl group, optionally substituted 1,3-dioxolane-2-yl group, Optionally substituted 1,3-dioxane-2-yl, Requires substituted 1,3-oxazolidin-2-yl, optionally substituted 1,3-oxazaperhydroin-2-yl, optionally substituted 1,3-dithiacenane-2-yl, optional Requires substituted 1,3-dipyrimidin-2-yl, alkoxycarbonyl, alkylaminocarbonyloxy, alkylaminocarbonylamino, 90038 -28- 200427680 dialkylaminocarbonylamino, alkylamine (Thiocarbonyl) amino, dialkylphosphoryluronium, optionally substituted pyrimyl, optionally substituted 3-, oxazolylalkoxy, optionally substituted aryl, optionally Requires substituted aryloxy, optionally substituted aryloxyalkyl, optionally substituted arylaminocarbonyloxy, optionally substituted heteroaryl, optionally substituted heteroaryloxy, Substituted pyrhakiyl as needed, substituted pyrazolyl as needed, substituted pyridoxy as needed, substituted 1,3-oxazoline as needed, substituted 1,3 as needed _Oxazolineoxy, optionally substituted 1,3-oxazolinylamino, optionally substituted 1,2,4-triazolyl, optionally substituted 1,2,3-thiazyl Diazolyl, as needed Substituted for 1,2,5-fluorenedifluorenyl, substituted if necessary 丨, 2,54 oxadiazolyl, substituted 2H-tetrayl as needed, substituted pyridyl as needed, as required Substituted pyrimidinyloxy, optionally substituted pyrimidinyl, optionally substituted pyrimidinyl, optionally substituted pyrimidinyloxy, optionally substituted 3,4,5,6-tetrahydropyrimidine Oxy, optionally substituted pyridineoxy, or optionally substituted tetrahydronaphthyl, where the I substituent is optionally selected from-or more than one halogen, alkyl, haloalkyl, The prerequisites for alkoxy, dialkoxyalkyl, dithioalkoxyalkyl, cyano, nitro, amine or alkoxycarbonylamino are at least one of r22, r23, R24, R25 and R26 is not hydrogen; when s is 1; E is selected from (CRURMh ^ CRMj ^ o, f 27 28, 3〇K) y, (CR27R28) x- (CR29R30) y〇 *, C 3 Η 6, C 4 Η 8, C! (= Ο), p 疒 ~ ^

; C (^ 0) C2H4 * &gt; C2H4C (-〇) * ^ C3H6C (= 〇) *, C4H8NHC (= 〇, * ten p) or Cos) NH * bridge base, of which the asterisk is 90038, 29- 427680 represents the next point of R8, where x is 1, 1; y is 0 or 1; and R27

, R28, R29, and R are independently selected from hydrogen, alkyl, and aryl substituted with, if necessary, j: complete oxy; ~ oxides; and agriculturally acceptable salts thereof. The present invention also relates to a composition comprising an insecticidally effective amount of at least one compound of formula 丨 and, if necessary, an effective amount of at least one second type compound and at least one agriculturally acceptable extender or adjuvant. The present invention also relates to a method for controlling insects where control is desired, which comprises applying an insecticidally effective amount of the above composition to a crop site or other area where insects are present or expected. Other aspects of the invention will become apparent. [Embodiment] An aspect of the present invention relates to a specific novel and useful compound, that is, a specific novel N- (substituted arylmethyl) -4- (disubstituted fluorenyl) as described in Formula I Hexahydro p-pyridine and p-pyridine derivatives ...

R 90038 -30- 200427680 where: m, η, q, r and s are independently selected from 0 or 1; and p is 0, 1, 2 or 3; A is selected from C and CH to form hexahydropyridine , 1,4-dihydropyridine and 1,2,5,6-tetrahydropyridine 6-membered acrophin ring; R2, R3, R4, R5 and R6 are independently selected from hydrogen, halogen, alkyl, and halogen Group, hydroxy, alkoxy, 1S alkoxy, pentathio, alkylthio, cyano, nitro, alkylcarbonyl, alkoxycarbonyl, aryl or aryloxy, the prerequisites are at least one of R2 , R3, R4, R5 and R6 are not hydrogen; and or take R2 and R3, or take R3 and R4 and -〇CF2〇-, -〇CF2CF2-, -CF2CF2〇- or -CH = CHCH = CH --- Benzo fused ring; and when (3) 111 and 11 are 0; then a double bond is formed between the methyl carbon (a) and the 4-position of the 6-membered acryl ring,

B R2 where B is phenyl substituted with R9, R10, R11, R12 and R13,

90038 -31-200427680 of which R, R, R, R12 and R13 are independently selected from hydrogen, halogen, alkyl, halogen, J: endyl, meridyl, alkoxy, self-alkoxy, sulfhydryl and alkane Thio, cyano, benzyl, pitoxycarbonyl or aryloxy; and either R9 and R1 Q, or R10 and R11 together with -〇CF2〇-, -〇CF2CF2- or -CF2CF2〇 to form benzene Fused ring; and (b) when m is 1 and η is 0; then a double bond is formed between the methyl carbon (a) and the 4-position of the 6-membered acyl ring,

Where B is a bridging group from methyl carbon (a) to R; where B is selected from 〇, S, * CH2〇, * 〇CH2, 〇C (= 〇) 〇, * OC (= 〇) NR15, * NR15C (= 0) 0 &gt; * OC (-S) NRl5 &gt; * NR15C (= S) 0 &gt; * 0CH2C (= 0) NR15, * NR15C (= 〇) CH20, * CH2〇C (= 〇) NR15, * NR15C (= 〇) 〇CH2, * NR15CH2, * CH2NR15, * NR15C (= 〇), * C (= 〇) NR15, * NR15S02, * S〇2NR15, * NR15NHS〇2, * S〇2NHNR15, * 0C ( -0) NRl5S02, * S〇2NR15C (= 〇) 0, * 〇C (= 0) NR15 90038 -32- W0427680 IHR ^ * CHR16NR16C (= 0) 0 ^ NR15C (= 0) NR16 &gt; Oxycyclohexyl Or 4-oxyhexahydropyridine-butyl, where the asterisk represents the point of attachment to the methyl carbon; W and R16 are independently selected from hydrogen, fluorenyl, ammonium carbonyl, and arylcarbonyl, where aryl Substitute with halide, alkyl, alkoxy, alkyl, alkoxy, or nitro if necessary; where R is pit, cyclohexyl, fluorenyl, or alkynyl; or R is R17 , R18, R19, R2G and R21 substituted phenyl;

Or R is pyridin-2-yl substituted with R18, R19, R20 and R21;

Or pyridin-3-yl substituted with R17, R19, R20, and R21 90038 -33- 200427680 R17

R20 or orbipyridin-4-yl substituted with R17, R18, R20 and R21; R17

R ′ or pyridin-3-yl substituted with Ri9, R20 and R21;

Wherein R17, R18, R19, R2G and R21 are independently selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, ialkylthio, cyano, nitro, and alkane Carbonyl, alkoxycarbonyl, alkoxycarbonylamino, aryl, aryloxy, and 2-alkyl-2H-tetrazole, and either R17 and R18, or R18 and R19 can be used with -CH2CH = CHCH2 -, -〇CF2〇-, -OCF2CF2- or -CF2CF2C)-form a benzo-fused ring; and at 90038 -34-200427680 (c) m and η system 1; Forms a single bond with the 4-position of the 6-membered acryl ring,

Where B is a bridging group from methyl carbon (a) to R; where B is selected from 〇, S, * CH20, * 〇CH2, 0C (= 0) 0, * 0C (= 0) NR15, * NR15C (= 〇) 〇, * 〇C (= S) NR15, * NR15C (= S) 0, * OCH2C (= 〇) NR15 ^ * NR15C (= 0) CH20 &gt; * CH20C (= 0) NRl5 &gt; * NR15C ( = 0) 〇CH2, * NRi5CH2, * CH2NR15, * NR15C (= 0), * C (= 0) NR15, * nr15so2 &gt; * so2nr15 ^ * NRl5NHS〇2 ^ * so2nhnr15 &gt; * 〇c (= o) nr15s〇2, * s〇2nr15c (= o) 〇, * 〇c (= 〇) nr15chr16, * CHR16NR16C (= 0) 0, * NR15C (= 0) NR16, 1,4-dioxocyclohexyl or 4- Oxygen ττ hydrogen p ratio -1-yl 'where the asterisk represents the point of attachment to methyl carbon (a); where R15 and R16 are as described above; and R-based alkyl, cycloalkyl, dilute or alkyl Talking about the base; or R is a stupid group substituted with R17, Ru, R19, R2Q and R21; pyridin-2-yl substituted with Ri8, R19, 90038 -35-200427680 R20 and R2 !; R17, R19, R2Q and R2! Substituted pyridin-3-yl; pyridin-4-yl substituted with R17, R18, R2G, and R2 !; or pyridin-3-yl substituted with R19, R20, and R21; where R17, R18, Ri9, R20 and R21 are described above; R1 is selected from hydrogen , Alkyl, alkoxyalkyl, or aryl; when p is 1, 2, or 3; then D is -CH2- and forms an azabicyclic derivative of a 6-membered acryl ring; when q is 0 and When r is 1, it is a 6-membered nitrogen ring nitrogen oxide derivative; when q is 1 and r is 0 or 1, R7 is selected from alkyl, haloalkyl, alkyl, and alkyl Oxyalkyl, dialkylaminoalkyl, alkylaminocarbonyloxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, alkcarbonyloxyalkyl, alkoxycarbonylalkyl, carboxy Alkyl, aralkyl, arylcarbonyl, sulfonate, or sulfonate alkyl groups, and can carry a negative charge to form internal salts; and separate ionic chlorides, bromides, iodides, or sulfuric acid or alkyl sulfonates or Phenyl ester; when s is 0 or 1; R8 is selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkoxy, alkoxyalkyl, amine, morphoyl, and Substituted pyrene, six-leaf dyneinyl, substituted (p than pyridyl) alkenyl, substituted 1,2,3,4-tetrahydrofluorenyl if necessary, substituted as necessary Of arylpyrazolyl, benzo [b] p-phenylenyl, 5-hydrogenated p-pyrido [l, 2 a] p dense group, optionally substituted 4-hydro-1,3_oxazolino [3,24pyrimidinone group, 1,2,3,4_tetrakis p 17 2-thio-1,3-dihydrop-quinolinol, 1,3-dihydrop-quinolinyl, or benzo [c] azepinedione, with optional substitutions The base system is 90038 -36- 200427680 halogen, alkyl, alkoxy and nitro; or R8 is phenyl substituted with R22, R23, R24, R25 and R26, R22

R23 R24 9 or pyridin-2-yl substituted with R23, R24, R25 and R26;

Or pyridin-3-yl substituted with R22, R24, R25 and R26; R22

R or pyridin-4-yl substituted with R22, R23, R25 and R26; R22

R25 -37- 90038 200427680 of which

R22, R23, R24, R25 and R26 are independently selected from the group consisting of hydrogen, halogen, alkyl, hydroxy, tigeroxy, alkoxy, dioxoyl, dioxoyl, and alkoxyimine Alkylalkyl, alkenoxyiminoalkyl, alkynoxyiminoalkyl, cycloalkylalkoxy, alkoxyalkoxy, alkylthio, dithioalkoxyalkyl, trisulfide Alkenyl alkynyl, alkynyl sulfonyl, alkynyl sulfonyl @ 1 radical, dialkyl sulfonyl sulfonyl, cycloalkynyl amine fluorenyl, alkenyl, block oxy, i-enoxy, Alkylsulfonyloxy, optionally substituted arylalkyloxy, cyano, nitro, amine, alkylamino, alkylamino, alkyloxycarbonylamino, alkenyloxycarbonylamino , Alkynyloxycarbonylamino, haloalkylcarbonylamino, alkoxyalkoxycarbonylamino, (alkyl) (alkoxycarbonyl) amino, alkylsulfonylamino, optionally substituted (Heteroaryl) (alkoxycarbonyl) amino group, optionally substituted arylcarbonylamino group, formamyl group, optionally substituted 1,3-dioxolane-2-yl group, and optionally Substituted 1,3-dioxane-2-yl, as Requires substituted 1,3-oxazolidin-2-yl, optionally substituted 1,3-oxazaperhydroin-2-yl, optionally substituted 1,3-dithiacenane-2-yl, optional Requires substituted 1,3-dithian-2-yl, alkoxycarbonyl, alkylaminocarbonyloxy, alkylaminocarbonylamino, dialkylaminocarbonylamino, alkylamino (thiocarbonyl) Amine group, dialkyl phosphoureido group, substituted thienyl group if necessary, substituted 1,3-thiazolyl alkoxy group if necessary, substituted aryl group if necessary, substituted aromatic aryl group if necessary Group, optionally substituted aryloxyalkyl group, optionally substituted arylaminocarbonyloxy group, optionally substituted heteroaryl group, optionally substituted heteroaryloxy group, optionally substituted pyrrole As needed, substituted pyridine 90038 -38- 200427680 oxazolyl, substituted pyrenyloxy as needed, substituted as needed 丨, heptamyl, substituted linoxy as needed, as needed Substituted 1,3-oxazolinylamino, optionally substituted1,2,4-diazolyl, optionally substituted 1,2,3-thiadiazolyl, optionally substituted 1 2,5-thiadiazolyl, optionally substituted I, 2,5-thiadiazolyloxy, optionally substituted 2H-tetrazolyl, optionally substituted alkyl, optionally substituted Pyridyloxy, optionally substituted amines, optionally substituted yodo groups, optionally substituted 17 melamine groups, and optionally * substituted 3,4,5,6-tetra Hydropyrimidinyloxy, optionally substituted glutamyloxy, or optionally substituted 1,2,3,4-tetrahydrothethyl, wherein the optional substituent is selected from one or more , Alkyl, i-alkyl, alkoxy, dialkoxyalkyl, dithioalkoxyalkyl, cyano, nitro, amine, or alkoxycarbonylamino, the prerequisites are at least one of them R22, R23, R24, R25 and R26 are not hydrogen; when s is 1; E is selected from (CR27R28) x- (CR29R30) y, (CR27R28) x- (CR29R30) y〇 *, C3H6, C4H8, C ( = 〇), c (= 0) C2H4 *, C2H4C (= 0) *, C3H6C (= 0) *, C4H8NHC (= 〇) *, or C (= S) NH * bridge base, where the asterisk represents the base of R8 Next point, where X is 1; y is 0 or 1; and R27, R28, R29 and R are independently selected from the group consisting of alkoxy Group substituted murine, tigeryl and aryl groups; 90038 -39- 200427680 N-oxides; and agriculturally acceptable salts thereof. Compounds of particular interest within the scope of the present invention are those in which p and q are 0; r is 0 or 1 and s is i; R2, R3, R4, "and" are independently selected from hydrogen, halogen, alkyl, Haloalkyl, hydroxyl, alkoxy, self-alkoxy, pentahalothio, alkylthio, nitro, aryl, and aryloxy; £ (Cp ^ R28) ^ (CR29R3G) y- bridging group (Where X is 1 and y are 0, R27 and R28 are hydrogen); and r8 is phenyl substituted with R22, R23, R24, R25 & R26, wherein r22, r23, R24, R25 and R26 are independently selected from hydrogen , Alkoxy, dialkoxyalkyl, dithioalkoxyalkyl, alkoxyiminoalkyl, alkenoxyiminoalkyl, blockoxyiminoalkyl, alkoxy Carbonylamino, optionally substituted arylcarbonylamino, :): complete oxycarbonyl, carbamoyloxy, optionally substituted dioxolane-2-yl, optionally substituted i, 3-dioxane-2-yl, optionally substituted 1,3-dipyrimidin-2-yl, optionally substituted 1,3-dithiazane-2-yl, if necessary Substituted aryl, optionally substituted aryloxy, optionally 2H -Tetrazole, optionally substituted pyridyl, optionally substituted pyridyloxy, optionally substituted pyrimidinyl, optionally substituted p-methoxy, and optionally substituted pyridyloxy. In one aspect of the present invention, preferred compounds of the present invention are those in which A is C and forms a hexahydro alpha ratio ring; m is (a) 0 or (b) l and η is 0, at methyl carbon ( a) A double bond is formed with the 4-position of the hexahydroρ ratio ring; and (a) when m and η are 0; 90038 -40- 200427680 B is replaced by R9, R10, Ru, Ri2 &amp; Ri3 Phenyl, wherein r9, ri0, R11, R12, and R13 are independently selected from hydrogen, halogen, alkyl, haloalkyl, hydroxy, alkoxy, self-alkoxy, sulfhydryl, and alkylthio; or When (b) m is 1 and n is 0; B is a bridging group selected from 0, * 〇 (: 〇 州 1115 and * S02NR15, where γ is hydrogen; and R is R17, R18, R19, R21R2i Substituted phenyl, wherein r17, ri8, R19, R ′ and R21 are independently selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, aryl, aryloxy and 2-Alkyl-2H-tetrazole. Those in which R2, R3, R4, R5, and R6 are independently selected from hydrogen, sulfonium, alkynyl, and halo * oxy; and R22, R23, R24, r25 and r26 is independently selected from hydrogen, dialkoxyalkyl, dithioalkoxyalkyl, alkane Alkyliminoalkyl, alkylaminocarbonyloxy, optionally substituted 1,3-dioxolane, optionally substituted 1,3-dioxane-2-yl, optionally Substituted aryloxy group, optionally substituted 2H-tetrazole, optionally substituted pyridyloxy group, optionally substituted pyrimidinyl group, optionally substituted pyrimidinyloxy group, and optionally substituted Pyridoxy compounds are more preferred. Those i) wherein (a) m and η are 0; and R9, Ri0, ru, Ri2, and r13 are independently selected from hydrogen, halogen, haloalkyl, and haloalkoxy ; Where R2, r3, R5, R6, R9, R1. , R12, R13, R22, r2, are more special for hydrogen; R4 and Rh are difluoromethyl, trifluoromethyl, or trifluoromethoxy; and R24 90038 -41-200427680 Compounds based on stilbene or pyrimidin-2-methyl are particularly preferred. Others injtcb / u, — 肀 (b) m system 1 and n system 〇; b system 〇 or * 〇c 卜 〇) NR1: bridging base; and RI7 丨 8, R, R and R "are independent Selected from hydrogen, halogen, haloalkyl, and halooxy; where R2, R3, R5, R6, R17, R! 8, R20, R 2 丨, 2 2 23, R, R2 &quot; and R26 are hydrogen Especially; R4 and R19 are difluoromethyl and oxy compounds.

-Murine methyl or trifluoromethoxy; and r24 is pyridine. 2-oxy or pyrimidine I. Someone's. In another aspect of the invention, the preferred compounds of the invention are those Wherein A is CH to form a hexahydropyridine ring; (c) m and n are 1 ′ to form a single bond between the methyl carbon (a) and the position of the ring; R1 is hydrogen; B is selected from 0, * 〇C (= 0) NR15 and * s〇2NR15 bridging group, in which R15 is hydrogen; and R is R17, R18, R19, R20 and substituted phenyl, in which Rn, ri8, R, R2G and R21 are independent It is selected from the group consisting of hydrogen, halogen, fluorenyl, haloyl, alkoxy, carbamo, nitro, square, aryloxy, and 2-carbyl-2H-tetrafluorene. To those in which R2, R3, R4, R5 and R6 are independently selected from hydrogen, halogen, haloalkyl and haloalkoxy; and R22, R23, R24, R25 and R26 are independently selected from hydrogen, dialkoxyalkane Group, dithioalkoxyalkyl group, alkoxyiminoalkyl group, alkylaminocarbonyloxy group, optionally substituted, 3-dioxolane, substituted if necessary, 3-, Dioxane hexadecyl, optionally substituted aryloxy, optionally substituted 2Ηβtetratidine, optionally substituted P than oxy, substituted pyrimidinyl, optionally substituted Pyrimidinyloxy and 90038 -42- 200427680 Compounds substituted with pyridoxy as required are more preferred. With those 8 series 〇 or * 〇C (= 〇) NR 丨 5 bridge groups; R17, R18, R19, R and R are independently selected from the group consisting of hydrogen, halo, halo and halooxy,

R R, R5, R6, r1 R1

R 2〇, R 2i, R 22, and R 23 HR 2 are particularly preferably hydrogen; 4; R, R 19 are difluoro f-based, trifluoromethyl or trifluoromethoxy, and R are pyridine_2-oxy or pyrimidine_2_oxy Base compounds are particularly preferred. In the special case 6, the compound within the formula may have an asymmetric center, which may cause optical enantiomers and diastereomers. Compounds in the range of Formula 丨 can exist in two or more types, that is, polymorphs, which have significantly different physical properties and chemical properties. Compounds in the range of formula I may also exist as tautomers with equilibrium. The compounds within the formula may also have acidic or basic moieties, which may allow them to form agriculturally acceptable salts or agriculturally acceptable metal complexes. The present invention includes these enantiomers, polymorphs, tautomers, salts and yttrium metals. Agriculturally acceptable salts and metal complexes include, but are not limited to, for example, ammonium salts, salts of organic and inorganic acids (such as hydrochloric acid, sulfonic acid, ethyl 70 ^ monofluoroacetate, methyl ester (Acids, phosphoric acid, gluconic acid, dibenzyl I and other acid salts), and alkali metal and alkaline earth metal complexes (for example, with sodium, potassium, lithium, magnesium, calcium and other metals). According to the present invention, the effective amount of the compound of formula 1 in the insect insect system appears in the range of insects to kill or control the insects. The preferred insecticidal effectiveness is those that are sufficient to kill insects. Within the scope of the present invention, the compound of formula I appears in insect pupae 15 by contacting the insect with a derivative of the compound, and the derivative is converted into the compound of formula Z in the insect. The invention includes applications of these compounds 90038-43-200427680, which may be referred to as proto-insecticides. Another aspect of the present invention is a combination of an insecticidally effective amount of at least one dilute Formula I compound and, if necessary, an effective amount of at least one second class compound and at least one agriculturally acceptable extender or adjuvant Thing. Another aspect of the present invention relates to a method for controlling insects, which is applied to a crop site (such as cereals, cotton, vegetables, and fruits, but not limited thereto) with an insecticidally effective amount of the above-mentioned composition. ) Or other areas' or adjacent areas where insects are present or expected. The invention also includes the use of the compounds and compositions described herein for controlling non-agricultural insect species (e.g., ants, dried wood termites and terrestrial termites and other insects), and also as pharmaceutical agents and compositions thereof Its application. In the veterinary medicine page 7 domain towel, the compound of the present invention is effective against special internal and external parasites, such as insects and podless parasites. Examples of certain animal parasites include, but are not limited to, gastronomy, sphaerocephalus, canine lice, stinkworm, cat flea, and other species. Acknowledges that the terms used in the substituents and used separately as part of the hydrazone, unless otherwise stated, are 垸, π, π, π, π, π, π, 垅, 垅, 垅, 垅, 垅 垅, 其, 垅, 垅, 垅, 基, 其Oxygen &quot; and &quot; Block oxygen π preferably includes a straight or branched chain which is suitable as a substituent, and from up to 12 carbon atoms 1, T soil has 10 carbon atoms More preferably, up to 7 carbon atoms are the best, "T group" and ^ carbon to 俨 "earth y a carbon to carbon double bond and" alkynyl "has at least one dead reference bond." 其 I " Divided ... x ring structure, uT ~ refers to aromatics with 4 to 10 hard atoms refers to 戸 裯 &quot;%, for example, phenyl and naphthyl. "Heteroaryl" One or more atoms in the term coat are not carbon (eg, sulfur, oxygen, or nitrogen) 9038-44- 200427680 including fused rings. "THF ·" has 4 to 10 The aromatic ring structure DMF of each carbon atom refers to fluorine, and the term refers to tetrahydrofuran. "DMSO" refers to methyl sulfoxide. ,, and the term refers to N, N-dimethyl Tamine. " , Or, dentate, the term line / acupoint, Qi or chlorine. g abbreviate ambient temperature &quot; 戋, room temperature &quot; to &quot; rt &quot;, for example, when referring to the temperature of the chemical reaction mixture ', it means in the range of 20t to 30T: Within the temperature. The compounds of formula I of the present invention can be synthesized from intermediates readily available on the market by methods known individually to those skilled in the art. The following Scheme 1 illustrates the general steps used to synthesize those compounds of Formula I, where A is C to form a hexahydropyridine ring; η is 0, between the methyl carbon (a) and the 4-position of the hexahydropyridine ring Form double bonds; m, p and q are 0; 1 * system 丨 form N-oxide; and S system 1; E system-(CR27R28V (CR29R30) y_ (where read "and y system 0); R8 is based on R22, r23, R24, R25 and R26 substituted phenyl; B is a phenyl substituted with R9, R10, R11, RllRl3, where R27 and R28 are hydrogen: Scheme 1 90038

In which R24 is not a substituent of hydrogen -45- 200427680

R3 provides a compound of formula I in which R24 is, for example, -NHC〇2C2H5, and r and q are 0

h5c, oxhn „F as a compound of formula I above is converted to its N-oxide in which r is 1 and q is 0

Compound of formula c) CF3COOH / 70 ° C; d) K, Co3 / EtOH / 25-75 ° C; e) / 5% Pt-carbon / EtOH / HOAc / 75 ° C;

jLH2 / Fe / EtOH / HOAc / 65 ° C; k) C2H5C02C! / EtOAc / 0-5 ° C; h) 30% H2〇2 / Me〇H In the first step described in Scheme 1, the Appropriately substituted methanol (c) (e.g., 4- {bis [4- (trifluoromethyl) phenyl] hydroxymethyl} hexahydropyridine) is treated with trifluoroacetic acid under reduced temperature to produce the corresponding unsaturation Methylene derivative (D) (for example, 4- {bis [4- (trifluoromethyl) phenyl] methylene} hexahydropyridine). The intermediate (D) is then reacted with a suitably substituted phenyl bromide (for example, 4-nitrophenylmethyl bromide) under basic conditions and in a suitable solvent to provide a 1-substituted pyridyl derivative ( E) (e.g., 4- {bis [4- (trifluoromethyl) phenyl] fluorenidyl 1-[(4-nitrophenyl) methyl] hexahydropyridine). The intermediate (E) is then hydrogenated in the presence of a catalyst (for example, 5% palladium-carbon) and at an elevated temperature, thereby reducing the nitro group to an amine group, providing 4-[(4- {bis [( Trifluoromethyl) phenyl] methylene} hexahydropyridyl) methyl] phenylamine (F). The intermediate (F) is sequentially reacted with an alkyl haloformate (for example, ethyl chloroformate) under basic conditions and in a suitable solvent to provide the corresponding alkylcarboxamide, a compound of formula I (for example, N_ {Heart [('{bis [4- (trifluoromethyl) phenyl] methylene} hexahydropyridyl) methyl] phenyl 丨 ethoxycarboxamide). The thus prepared carboxyamidamine is then treated with 30% 90038 -46- 200427680 in methanol, for example, by emulsification hydrogen treatment to convert it into the corresponding oxyoxyhydroxyl derivative (N-oxide), providing Additional formula compounds. A detailed example of this synthesis step is provided as an example described below. The following scheme 2 illustrates the general steps used to synthesize those compounds of formula j, where A is CH to form a hexahydropyridine ring; η is 1 to form a single bond from methyl carbon (a) and its derivatives; p, q And r are 0; m and s are 1; B is a bridging group from methyl carbon to R; E is-(CR27R28) x- (CR29R3G) y- (where X is 1 and y is 0); R8 is based on R22, R23, R24, R25, and R26 substituted phenyl; and R is phenyl substituted with R17, R18, R19, R20, and R21, where R27 and R28 are hydrogen: Scheme 2

90038 47- 200427680 ^ 23 ^ 22

〇Mg / I2 / THF / &lt; 40 ° C; j) HC1 (g) / EtOAc; k) H2 / pt〇, / Me〇H. 〇NN diisopropylethylamine / DMSO; m) Et3N / CH7CI7 / 35 ° C_, In a synthesis as described in Scheme 2, the intermediate (ji) is first prepared by using appropriate formazan (for example, η α &quot; (4- (2-pyridoxine) Group) phenyl) formaldehyde) reacts with sodium borohydride at reduced temperature and in a suitable cereal, to produce a substituted fluorenol derivative (for example, anti-Kong Miao-pyridyloxy) Phenyl) f alcohol); 90038 200427680, which in turn reacts with thionine gas in the presence of a catalytic amount of pyridine at a reduced temperature and in an appropriate solvent to produce, for example, (4- (2-pyridyloxy) phenyl) Methyl chloride (J 1) In a second synthesis as described in Scheme 2, a suitable aldehyde (eg, 4-pyridinecarboxaldehyde) and a Gngnard reagent (eg, 'trifluoromethyl Phenylmagnesium bromide) is reacted at an elevated temperature and in a suitable solvent to produce a corresponding pyridinemethanol, for example, 4- (trifluoromethylphenyl) -4_pyridinemethanol (G). The intermediate (G) is then treated with a hydrogen chloride gas in a suitable solvent to convert it into the hydrochloride (H). The salt (H) thus formed is then hydrogenated in the presence of platinum oxide to supply the corresponding pyridyl methanol, for example, 4- (trifluoromethylphenyl) -4-pyridylmethanol hydrochloride (J) . In order to replace the 1-position of the π-hydropyridine ring, the intermediate (j) and the intermediate (H) are reacted under basic conditions and in an appropriate solvent to provide the corresponding methanol derivative (K) (for example, '{ 1-[(4_ (2-pyridyloxy) phenyl) methyl] (hexahexapyridyl)} [4- (digasmethyl) phenyl] methanol). The intermediate (κ) is then reacted with an appropriate isocyanate (for example, 4-chlorophenyl isocyanate) under basic conditions and in an appropriate solvent to provide the corresponding compound, a compound of formula I (for example, chlorophenyl) ( {1-[(4- (2-p ratio hydroxy) phenyl) methyl] (4-hexahydrop ratio phenyl) 丨 [4_ (trifluoromethyl) private] methoxy) amine). Example 2 described below provides detailed steps for this synthesis. The carboxyamidide thus prepared as described in Example 2 is treated with, for example, 50% hydrogen peroxide in a suitable solvent to convert it to the corresponding oxyoxy group: ^ hydrogen p-ratio derivative (N-oxide ). Example 6 described below provides detailed steps for this synthesis. A similar compound was prepared using similar procedures as described in Scheme 2, wherein A is C, forming a 1,2,5,6-tetrahydropyridine ring. Example 5 described below provides detailed steps for this synthesis. 90038 -49- 200427680 The following scheme 3 exemplifies the general steps for the synthesis of those compounds of formula I, where A is CH ′ to form hexa-argon oxide / depletion; η is to be formed from methyl charcoal ( a) and its derivatives · p, q and r are 0; m and s are 1; B is a bridging group from methyl carbon to R; E is-(CR27R28) x- (CR29R30) y- (Where X is 1 and y is 0); and R8 is phenyl substituted with R22, R23, R24, R25, and R26; wherein R27 and R28 are hydrogen: Scheme 3

Among them, R22, R23, R25 and R26 are hydrogen, refer to Example 19 of US Patent No. 5,639,763.

90038 -50- 200427680

q) Ν, Ν-, diisopropylethylamine / DMSO; r) NaOH / H20 / MeOH / THF; s) (Et〇) 2P (0) CN / HN (0CH3) (CH3): HC1 / DMF / 0 ° C; t) Mg / THF / RT-60 ° C; v) H2N〇H: HC1 / Et3N / Et〇H / reflux; w) LiAlH4 / THF / RT-63 ° C; x) C3H7S02C1 / Et3N / CH2C12_ 90038 -51-200427680 As described in Scheme 3, 'known compounds (for example, 5- [4- (bromomethyl) phenyl] -2-methyl-1,2,3,4-tetrasial ( )) Reacts with isonapic acid (isoponic acid ethyl ester under basic conditions and appropriate solvents to provide the corresponding cool (p) (for example, l-{[4- (2-methyl- i, 2,3,4-tetrazol-5-yl) phenyl] methyl} hexahydropyridine-4-carboxylic acid ethyl ester), which are reacted with aqueous sodium hydroxide in a suitable solvent and sequentially converted Into its hexahydropyridinecarboxylic acid (Q), providing for example; μ {[4- (2-methyl-1,2,3,4-tetramethyl-5-yl) phenyl] methyl} hexahydroρ ratio Dianjun acid. Then the intermediate (Q) is reacted with, for example, N, 0-dimethylhydroxylamine hydrochloride and diethyl cyanophosphonate under basic conditions, under reduced temperature, and in an appropriate solvent. Generates the corresponding hexahydroxanthenylcarboxamide (R) (example , 1-{[Heart (2-methyl (1,2,3, oxotetrazol-5-yl)) phenyl] methyl} (4-hexahydropyridyl) -N-methylcarboxamide) The intermediate (R) is reacted with a Grignard reagent (for example, 4-trifluoromethoxyphenylmagnesium bromide) in an appropriate solvent to provide a corresponding ketone (Tχ, for example, 2-methyl (1 , 2,3,4-tetrakis-5-yl)) phenyl] methyl} (4-hexahydroρ bisyl) 4- (trisylmethoxy) phenyl ketone). The intermediate (T) is sequentially reacted with hydroxylamine hydrochloride at an elevated temperature, under basic conditions, and in a suitable solvent to produce a corresponding hydroxyimino (U) intermediate (for example, (hydroxyl Imino) (1-[[4- (2-methyl (1,2,3,4-tetra-5-enyl)) phenyl] methyl] (4-hexahydrop-specific group) [4 -(Trifluoromethoxy) phenyl] methane). The intermediate (U) is then reacted with, for example, lithium aluminum hydride and then with ammonium chloride in a suitable solvent to provide the corresponding amine (V) derivative ( For example, '1-[[4- (2-methyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl] (4-hexahydrocarbyl)) [' (Three Fluoromethoxy) phenyl] methylamine). The amine (v) is sequentially reacted with an appropriate || compound (e.g., μpropanesulfonyl chloride) under basic conditions and in an appropriate solvent to provide a compound of formula I (for example, [(1-{[4- ( 2-methyl 90038 -52- 200427680 (1,2,3,4-tetrasal-5-yl)) phenyl] methyl} (4-hexahydro leaf |: bitenyl)) [4_ 三 气 甲(Oxy) phenyl] methyl] propylsulfonaminium). Example 3 described below provides detailed steps for this synthesis. The following Scheme 4 illustrates another general step for the synthesis of those compounds of the formula wherein A is CH to form a hexahydropyridine ring; η is 1 to form a single bond from methyl carbon (a) and its derivatives; p , Q and r are 0; m &amp; s is 1; β is a bridging group from methyl carbon to R; E is-among which is 1 and y is 0); and R8 is R22, R23, R24, Rh &amp; R26 substituted phenyl; wherein R27 and R28 are hydrogen: Scheme 4

90038 -53- 200427680

Compound of formula I y) Mg / THF / 40 0C; z) HC1 (g) / Et20; aa) H2 / Pt02 / MeOH; bb) N, N-diisopropyl ether / DMSO; cc) NaH / PMSQ / 85-90 ° C, as described in Scheme 4, 'Cyanopyridine (w) (for example, 4-cyanopyridine) and Griya reagent (for example, 4-trifluoromethoxyphenyl magnesium bromide) Reaction in an appropriate solvent, the corresponding ketone (x) (for example, 4-pyridyl 4- (trifluoromethoxy) phenyl ketone) is supplied, and it is reacted with hydrochloric acid gas in an appropriate solvent, and sequentially converted To its hydrochloride (Y). The intermediate (Y) is sequentially hydrogenated in the presence of platinum oxide and in a suitable solvent to provide the corresponding methanol (z) (for example, 'hexahydropyridyl [cardio (difluoromethoxy) benzyl] methanol) 'Hydrochloride). In order to replace the position of the ring of the hexahydro leaf, the intermediate (Z) and an appropriate methyl halide (for example, 5- [4-(&gt; stinky f7 group) winteryl] -2-methyl-1 , 2,3,4 -tetra wow) react under experimental conditions and in an appropriate solvent to supply the corresponding methanol (AA) derivative (for example, {1-[(2-methyl (1,2,3 , 4-tetramethyl-5-yl)) methyl] (4-TTchloroppyridyl)} [4- (trifluoromethoxy) phenyl] methanol). The intermediate (AA) is then treated with sodium hydride at elevated temperatures in sequence, and then reacted with an appropriate compound (for example, 2-fluoro-5-trifluoromethylpyridine) to provide a pyridine derivative, Compounds of formula I (for example, 2-[(1-{[4- (2-methyl (1,2,3,4-tetramethyl-5-yl)) phenyl] methyl 90038 -54- 200427680 group} (4-Hexahydroxyl)) [4γ: methyl) ρ ratio bite). Fluoromethoxy) phenyl] methoxy], 5, described in Example 4 below provides a detailed illustration of Scheme 5 under this synthetic step w, which is used for 小 小 small. . The general steps for those compounds of formula I, in which A is C, form hexahydropyridine. "Coat, η is 0 'formed between the methyl carbon (a) and the 4-position of the hexachloro p-pyridine ring Double bond; where B is a bridging group from methyl carbon to R; p, q and r are 0 ·, m and s are 1; E is-(CR27R28) x- (CR29R3 °) y- (where X is 1 And y is 0); R8 is a phenyl substituted with R22, R23, R24, R25, and R26; and R is a phenyl substituted with R17, Ri8, R19, R20, and R21; wherein r27 and R28 are hydrogen: Scheme 5

〇ch3 90038 200427680

n) NaN3 / NH4C1 / DMF / 140 0C; 〇) EtI / K2C03 / DMF; p) NBS / CC14 / loopback; q) N, N-diisopropylethylamine- / DMS0; r) Na0H / H20 / Me0H / THF; s) (EtO) 2P (〇) CN / HN (0CH3) (CH3): HC1 / DMF / 0 ° C; t) Mg / THF / RT-70 ° C * u) P〇ri / Ht2Q v) K2CO, / DMF____ 3 As described in Scheme 5, an intermediate is prepared by reacting an appropriate nitrile nitrile (e.g., para-enzyme nitrile) with sodium azide at an elevated temperature and in a suitable detergent. (M) (e.g. '5- (4-methylphenyl) -1,2,3,4-tetrasial). The intermediate (μ) is then fluorinated under appropriate conditions with an appropriate fluorenyl chain, and the corresponding fluorinated tetrafluorene (N) is supplied (for example, 2-ethyl-5- (4-methylbenzene). ))-1,253 54-tetrazole). The intermediate (N) is brominated in sequence with, for example, N-bromosuccinimide at an elevated temperature and in a suitable solvent to provide the corresponding bromomethyl derivative (0) (Example 90038 -56- 200427680 Such as 5 [4-(/ Kynyl) phenyl &gt; 2-ethyl-1,2,3,4-Tetracycline). The intermediate (0) is then reacted with ethyl isonapicate under basic conditions and in a suitable solvent to provide the corresponding ester (P) (for example, methyl ", 2,3,4-tetrazole 5 group) fluorenyl] methyl} a hydrogen p-Hydro-Pyronic acid 4-ethyl acetate), which is reacted with aqueous sodium hydroxide in a suitable solvent, and sequentially converted into its hexahydropyridinecarboxylic acid (Q) ′ Supply, for example, 1-{[4- (2-methyl-fluorene, 2,3,4-tetrazol-5-yl) phenyl] methyl} hexahydropyridinecarboxylic acid. Then, the intermediate (Q) and for example Ν, 〇_dimethylhydroxylamine hydrochloride and diethyl cyanophosphonate react under basic conditions, under reduced temperature and in a suitable solvent to produce the corresponding hexahydropyridinecarboxamide (R) ( For example, [4- (2-ethyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl} (analhexahydropyridyl) _normethoxy-N-methyl Methylamine). The intermediate (R) is reacted with a Grignard reagent (for example, 4-difluoromethoxyphenyl magnesium sulphide) in a suitable solvent to produce the corresponding iso (S) (for example , 1-{[4- (2-ethyl (ι, 2,3,4-tetrat-5-yl)) phenyl] methyl} (4-hexahydropyridyl)-(trifluoromethoxy ) Phenyl Ketone). The ketone 0 is then self-acylated with, for example, phosphonium chloride in a suitable solvent to produce the corresponding compound (S1) (for example, {4- [chloro group (1 _ {[4- (2-ethyl (1,2,3,4-Tetratyl-5-yl)) Epiyl] methyl} (4-ττ Biyodo)) methyl] phenoxy} trifluoro (methane). The intermediate ( S1) sequentially react with, for example, an appropriate phenol (such as 4- (trifluoromethoxy) phenol) in an appropriate solvent to provide a corresponding phenoxy derivative, a compound of formula I (such as' 1-[(1- { [4- (2-ethyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl} (4-hexahydropyridinyl)) [4- (trifluorofluorenyloxy ) Phenyl] methoxy] -4- (trifluoromethoxy) benzyl). Example 11 described below provides detailed details of this synthetic step. Examples 7, 8, 9 and 10 described below are provided in Those steps provided in Scheme 1_4 and the detailed synthetic steps of _38 -57- 200427680 dagger i compound prepared by methods derived from the examples of these schemes. Those skilled in the art will of course recognize the formulation of toxicants and Application patterns can affect the activity of a substance in a particular application. In other words, the insecticidal compound of the present invention can be formulated into particles having a relatively large particle size (for example, 8/1 6 or 4/8 US Mesh), water-soluble or water-dispersible particles, powdery powder, wettable powder, Concentrated emulsions, aqueous emulsions, solutions, or any other formulations known to be useful in agriculture, depend on the mode of application desired. Assuming that the word "about" is placed before the specified amount, then The amounts specified in this application are of course only approximate values. These insecticidal compositions may be sprayed with a spray or powder or granules diluted with water on the area where insect control is desired. These formulations may include active ingredients as small as 0.1 ° / 0, ο · 2% or 0.5% up to 95% by weight or more. Powder is a free-flowing active ingredient and finely divided solids (such as π stone powder, natural clay, diatomaceous earth, powdered materials (such as walnut cereal powder and cotton seed powder) and other organic and inorganic solids) used as a dispersant and carrier for poisons. Blends; these finely divided solids have an average particle size of less than about 50 microns. A typical monthly preparation formulation useful in this article is a private 1 fw bag, two, two, and rr g cb search g including 1. (knife I or less (insecticidal compound and 99.0 parts of talc) Powder formulations. Wettable powders (also useful formulations for insecticides) have a finely divided particle type that can be easily dispersed in water or other dispersants. The fishable powders are finally inferior to dry powders. ^, Or the place where the emulsion is sprayed in water or other liquids to control insects. The typical carriers of Wang Yizhi's meaning powder include Fuller's Gan, which can easily wet the inorganic diluent. Fuller's (Fuller , S) soil, kaolin clay, sand dioxide and its osmium: osmium absorbent. Made by Zhengtang, made by a positive suspension system, which contains about 5-80% active ingredients -58-_38 200427680 wet powder, which is based on the carrier Depending on the absorbency, and often also include a small amount of wetting agent, dispersant or emulsifier to accelerate dispersion. Example #, useful wettable powder formulations include 80_0 parts of insecticidal compounds, 17.9 parts of pamitol ( Palmetto) clay and __ amount of wooden sulphur Sodium and G.3 servings of acidified fatty anti-polyacetic acid as humectants. Additional humectants and / or oils that accelerate the dispersion on plant leaves are often added to synergistic mixtures. Other useful for insecticidal applications Is a concentrated emulsion (Ec), which is a liquid composition uniformly in water or other dispersants, and can be composed entirely of insecticidal compositions and liquid or solid emulsifiers, and can also include liquids. Carriers such as xylene, heavy aromatic naphtha, isophorone or other non-volatile organic solvents. For insecticidal applications, these concentrates are dispersed in water or other liquid carriers and are normally sprayed Apply to the area to be treated. The weight% of the basic active ingredient can be changed according to the way the composition is applied, but it usually contains 0.5 to 95% of the active ingredient by weight of the insecticidal composition. Water suspension Agent formulations are similar to EC, except that the active ingredients are suspended in a liquid Thai carrier (usually water). EC-like aqueous suspensions can include a small amount of surfactants and are typically included in combination The active ingredient in the range of 0.5 to 95% by weight is often from 10 to 50%. For application, the aqueous suspension can be diluted in water or other liquid vehicles, and is normally based on Spray Shili on the area to be treated. Typical wetting agents, dispersants or emulsifiers used in agricultural formulations include (but are not limited to) septic and thiosulfate _;): filling base and;) : The purpose of filling aryl g and their 90038-59-200427680, polyethylene oxide, sulfonic acid / free, fatty acid chain mercaptan of polyhydric alcohol, and scraping type of ethylene oxide are commercially available products. 1 to 5% by weight of the composition sodium salt, alkaryl polyester alcohol, sulfated high-carbon alcoholized animal and vegetable oils, sulfonated petroleum lubricants, and ethylene oxide addition products and long additions for these purposes product. Many other useful interfacial activities Normally when using surfactants, weight is included. The active ingredient in the solvent is propylene glycol or other suitable formulations which are suitable for inclusion in relatively non-volatile suspensions, such as in water, corn oil, kerosene, and solvents. Formulations that are useful for insecticidal applications include the active ingredient in a solvent (a simple solution, which is completely dissolved at the desired concentration, such as in propane, naphthalene, xylene, or other organic solvents. . Granule formulations (a carry poison 4 on relatively coarse particles) have a special atmospheric distribution or agricultural 2 mulch penetration applications. Pressurized sprays, typically aerosols, are used in which the active ingredients are dispersed into a finely divided form, thereby causing a low boiling point knife / combined carrier to burst out. Water-soluble or water-dispersible particles are free-flowing, dust-free and easily soluble or miscible particles. When farmers use granules, concentrated emulsions, concentrated aqueous suspensions, water emulsions, solutions, etc. on the field, they can be diluted with water to obtain the so-called 〇1% or 〇2% to 1.5% or 2 Active ingredient concentration in the range of%. The active insecticidal compound of the present invention may be formulated and / or sprayed with one or more compounds of the second type. These combinations can provide specific advantages, such as (unrestricted; this) exhibiting a multiplier effect on greater control of harmful insects, reducing the rate of application of insecticides, and thus reducing any environmental and worker safety 90038 -60-

200427bbU == :: A wider range of harmful insects, making agricultural plants more toxic to plants and improving resistance to non-harmful species such as mammals and fish. :: Class compounds include (but are not limited to) other pesticides, plant growth ::: materials, soil conditioners or other agricultural chemicals. When applying the activated mouthpiece of the present invention that is not formulated early, alone or with other agricultural chemicals, of course, an effective amount and concentration of the active compound is used. The range of 3 kg / ha changes to about 0. 03 to about i catty a soft and good. When applied to fields where insecticides are lost, higher application rates (for example, four times the above application rate) can be used. / The active insecticidal compound of the present invention is combined with-or a class II compound. When used orally, for example, in combination with other pesticides such as herbicides, the herbicides include, but are not limited to, for example: N- (phosphonocarboxymethyl) glycine ("Carfosin ( glyphosate) "), aryloxyalkanoic acids (such as (2,4 • dichlorophenoxy) acetic acid (" 2,4-D ,,), (4-chloro-2-methylphenoxy) Acetic acid (,, MCpA "), (+/-)-2- (4-chloromethylphenoxy) propionic acid (" MCPP ·, "); ureas (such as N, N-dimethyl-N , [4- (l -methylethyl) phenyl] urea ("isoproturon")); imidazolinones (such as 2 · [4,5-dihydro-4-methyl-4- (1-methylethyl) -5 -oxy-1 hydrazone -imidazol-2-yl] -3 -pyridinecarboxylic acid ("imazapyr")), containing (+ /-)-2- [4 , 5-dihydro-4-methyl-4- (1-methylethyl) -5-oxy-1H-imidazol-2-yl] -4-methylbenzoic acid with (+ /-) _ 2- [4 , 5-dihydro-4-methyl-4- (bumethylethyl) -5-oxy-1H-imidazol-2-yl] -5-methylbenzoic acid ("imazamethabenz" ) &quot;) reaction product, (+/-)-2- [4,5-dihydro-4-methyl-4- (1-methylethyl) -5-oxy- 1H-imidazol-2-yl] -5-ethyl-3-pyridine metabolite Γ imazethapyr '') and (+/-)-2- [4,5-dihydro 90038 -61-200427680 -4-methyl-4- (1-methylethyl) -5-oxy-1H-midoxan-2-yl] -3 -p-quinucleate Γ imazaquin &quot;) reaction product ); Diphenyl ethers (such as 5- [2-chloro-4- (trifluoromethyl) phenoxy] -2-nitrophenylarsinic acid ("acifluorfen &quot;), 5 -(2,4-dichlorophenoxy) -2-nitrobenzoic acid methyl ester (&quot; bifenoxn) and 5- [2-chloro-4- (trifluoromethyl) benzene Oxy] (methylsulfonyl) -2-nitrobenzimidamine ("fomasafen")); hydroxybenzonitrile (such as 4-mercapto-3,5-dihydroxyl) Bet ('· oxynil') and 3,5-dibromo-4-hydroxy (bromoxynil ")); sulfonylureas (such as 2- [ [[[(4-Chloro-6-methoxy-2-pyrimidinyl) amino] carbonyl] amino] sulfofluorenyl] benzoic acid (&quot; chlorimuron '·), 2- Gaso-N-[[(4-methoxy-6-methyl-1,3,5-trifluoren-2-yl) amino] carbonyl] benzenesulfonamide ("Chlorsulfuron (&amp; 〇111 (^ 111 to 1 * 〇11) | '), 2-[[[[[[[((4,6-dimethoxy-2-pyrimidinyl) amino] carbonyl] amino] sulfofluorenyl] methyl Phenyl] benzoic acid (π bensulfuron) ”, 2-[[[[[((4,6-dimethoxy-2-pyrimidinyl) amino] carbonyl] amino] sulfofluorenyl] methyl- lH-p Bijun-4-acid (pyrazosulfuron · *), methoxy-6-methyl-1,3,5-triphin-2-yl) amino] carbonyl] amine []] Sulfofluorenyl] -2_ Epiphenic acid (% Selenium 〇1 ^ € 6115111 € 111 &gt; 〇11) &quot;) and 2- (2-chloroethoxy)-; ^ _ [[(4 -Methoxy-6-methyl-1,3,5-tripent-2-yl) amino] anyl] benzoic acid amine ("tnasulfuron"))); 2 (4- Aryloxyphenoxy) alkanols (such as (+ /-)-2- [4-[(6-chloro-2-benzoxazolyl) oxy] phenoxy] propanoic acid Fenoxaprop'1), (+/-)-2- [4-[[5- (trifluoromethyl) -2-pyridyl] oxy] phenoxy] propanoic acid ('' Vorop (Fluazi fop) · '), (+/-)-2- [4- (6-Gasyl-2- and biting, lynyl) oxy] phenoxy) propionic acid (&quot; 禾 灵 (qUizai0f0p ) H) and (+/-)-2-[(2,4-dichlorophenoxy) phenoxy] Acid ("Heloline 90038 -62- 200427680 (diclofop)")); benzopyridones (such as 3- (1-methylethyl) -111-1,2,3-benzopyridine- 4 (3H) -one · 2,2 · dioxide ("bentazone")); 2-chloroacetamidine (such as N- (butoxymethyl) -2 -Chloro-N- (2,6-diethylphenyl) ethanamine Γ butachlor "), 2-chloro · N- (2-ethyl-6-methylphenyl ) -N- (2-methoxy-1-methylethyl) acetamide ("metolachlor"), 2-chloro-N- (ethoxymethyl) -N- (2- Ethyl-6-methylphenyl) acetamide ("acetochlor") and (RS) -2-chloro-N- (2,4-dimethyl-3-pyrimyl) -N- (2-methoxy-1-methylethyl) acetamide ("dimethenamide 1 ')); quinacids (such as 3,6-dichloro-2-methoxybenzene Formic acid dicamba 1 ')); pyridyl acetic acid (such as [(4-amino-3,5-dichloro-6-fluoro-2-oxoyl) oxy] acetic acid ( '' Fluroxypyr '')) and other herbicides. When the active insecticidal compound of the present invention is used in combination with one or more compounds of the second type, for example, in combination with other insecticides such as other insecticides, other insecticides include, for example, organic Phosphate insecticides (such as chlorpyrifos, diazinon, dimethoate, malathion, parathion-methyl, and terbufos); class Cordyceps insecticides (such as fenvalerate, deltamethrin, fenpropathrin, cyfluthrin, flUCythrinate, alpha-phenimerin cypermethrin), biphenthrin, cyhalothrin, etofenprox, esfenvalerate, tralomethrin, tefluthrin, beta Cypermethrin (cycloprothrin), β-sai funin and ananathrin) 90038. DOC -63-200427680; carbamate insecticides (such as aldecarb, carbaryl, carbofuran, and methodyl); organochlorine insecticides (Such as endosulfan, endrin, heptachlor, and lindane); benzene donkey urea insecticides (such as diflubenuron, triflunon ( triflumuron, teflubenzuron, chlorfluazuron, flucycloxuron, hexaflumuron, flufenoxuron, and lufenuron); and other insecticides (Such as amitraz, clofentezine, fenpyroximate, hexythiazox 'spinosad and imidacloprid) 〇 killing the activity of the present invention When an insect compound is used in combination with one or more compounds of the second type, for example, in combination with other pesticides such as fungicides, the fungicides include, for example, benzimid fungicides (such as raide ( benomyl), carbendazim, thiabenda zine) and thiophanate-methyl); 1,2,4-three-cooking fungicides (such as epoxyconazine, cyproconazine, and stone protection) flusilazine), flutriafol, propiconazine, tebuconazine, triadimefon, and triadimenol); substituted aniline fungicides (such as metronidazole ( metalaxyl), oxadixyl, procymidone, and vinclozolin); organophosphate fungicides (such as fosetyl, iprobenfos, and fencloxacin) (Pyrazophos), edifenphos and tolclofos-methyl); morphine fungicides (such as fenpropimorph, tridemorph, and diuron 90038 -64) -200427680 (dodemorph)); other comprehensive fungicides (such as fenanmol, imazaiu, pochiraz, three match spray (dagger 10; / (: 132 丨1 ^) and Seflon (^ 1 ^ 01411 €)); dithiocarbamate fungicides (such as zinc 4 mancozeb, Zhong Nai (Maneb), propmeb, zmeb and zinc dimethylamine (Zlram)); non-comprehensive slave elixir (such as chlorothaionii), Yifa Dichlofluanid, dithianon, iprodione, captan, dinocap, dodine, fluazinam, Giuazatine, pcnb, pencycuron, quintozene, tricylamide, and validamycm); inorganic fungicides (such as copper and sulfur Products) and other fungicides. When the active insecticidal compound of the present invention is used in combination with one or more compounds of the second type, for example, in combination with other insecticides such as nematicides, the nematicides include, for example: car | 3〇furan), butyl plus carbosulfan, turbufos, aldecarb, ethoprop, fenamph〇s, European kill ( Oxamyl), isazofos, cadusafos, and other nematicides. When the active insecticidal compound of the present invention is used in combination with one or more compounds of the second type, for example, in combination with other insecticides such as plant growth regulators, the plant growth regulators include, for example, statin hydrazide), chiormeqUat, ethephon, gibberellin, mepiqUat, orodiazepine (mabenfide, mabenfide) , Triaphenthen〇1, baksu 90038 -65- 200427680 (paclobutrazol), anacorna (unac〇naz〇1), dcpa, prohexadione, ethyl trinazate (Trinexapac-ethyi) and other plant growth regulators. Soil withering agents promote various kinds of shellfish that are beneficial to plant growth when added to the soil. Use of soil conditioning agents to reduce soil compaction, promote and increase effective drainage Properties, improve soil permeability, promote perfect plant nutrient content in the soil, and promote better insecticidal effects and fertilizer incorporation. The active insecticidal compounds of the present invention are combined with one or more second types When the composition is combined, for example, with other substances such as soil conditioners, the soil conditioner includes organic substances (such as humus) that promote the retention of cationic plant nutrients in the soil; mixtures of cationic nutrients (such as calcium, Magnesium, potassium feldspar, sodium and hydrogen complexes); or microorganic compositions that promote plant growth conditioning in the soil. These microorganic compositions include, for example, bacillus, Pseudomonas (psCDdom) Onas), nitrogen-fixing bacteria, azospirillum, rhizobium, and cyanobacteria. Fertilizers are cereal supplements that often include nitrogen, phosphorus, and potassium. In the combination of Ben Maoming's active insecticidal compound with one or more second class compounds, / f, ,, and, for example, combined with other substances such as fertilizers, the fertilizer includes nitrogen fertilizers (such as ammonium sulfate, Ammonium nitrate and bone meal); phosphate fertilizers (such as superphosphates, peroxoates, ammonium sulfate and diammonium sulfate); and potassium fertilizers (such as potassium chloride, sulfuric acid and potassium nitrate) and other fertilizers A further exemplifies the present invention by the following examples, but of course it should not be limited in any way. The examples are used to synthesize the compounds of formula i as shown in the formula 90038-66-200427680. Samples of the invention, a list of these synthetic species with examples, and specific biological data showing the effectiveness of these compounds. Example 1 This example illustrates the preparation of 1 {4-[(4- {bis [4- (trifluoromethyl) ) Phenyl] sulfenyl} hexahydropyridyl) methyl] phenyl} ethoxycarboxamide, N_oxide (compound 101 in the table below) step A as 4- {bis The synthesis effect of [4- (trifluoromethyl) phenyl] methylene} hexahydrogenated lake will be 105% in 50¾ liters of trifluoroacetic acid. A solution of 0 g (0.025 mol) of 4_ {bis [4- (trifluoromethyl) phenyl] light methyl} hexahydrop-bite (known compound) was heated to 70 ° C, and it was Stir for 4 hours. The excess trifluoroacetic acid was then removed by distillation. The residue from the distillation residue was added dropwise to ice water. At the end of the addition, the mixture was neutralized with a saturated aqueous solution of citric acid. Then, the mixture was taken in a gas-fired year, and the extract was washed with an aqueous solution saturated with gasified steel. The extract was concentrated to a residue under reduced pressure, and the residue was crystallized in hexane to give two yields of 9.1 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step B The synthesis of 4- {bis [4- (trifluoromethyl) phenyl] methylene} -1-[(4-nitrophenyl) methyl] hexahydropyridine as an intermediate will be carried out at about 20 3.8 grams (0. 010 mole) 4- {bis [4- (tri-n-methyl) phenyl] methylene} hexahydropyridine, 2. 2 grams (0. 010 mole) 4_nitrophenyl methyl bromide with 1. 7 grams (0. 012 mol) of potassium carbonate. The stirred mixture was warmed to 75 ° C and stirred for about 18 hours. Then another 0.2 g (0.001 mole) of 4-nitrophenylmethyl bromide and another 0.1 g 2 grams (0. 001 mole) potassium carbonate was added to the reaction mixture 90038 -67- 200427680. The reaction mixture was reheated to 75 [deg.] F: and stirred for about 8 hours. The reaction mixture was then cooled and filtered to remove excess potassium carbonate. The reaction mixture was then dissolved in acetic acid, and 0.2 g (catalyst) of 5% platinum-carbon was added to the next hydrogenation step. ¾ in the preparation of the mixture.臆 Measure the amount of the title compound. Step C The synthesis of 4-[(4- {bis [(trifluoromethyl) benzyl] methylene] hexahydropyridyl) methyl] phenylamine as an intermediate will come from the steps of the conventional examples The reaction product of B and 5% platinum-carbon in acetic acid were stirred at 75 ° C for about 18 hours, while hydrogen was bubbled into the reaction mixture. Analysis of the reaction mixture then showed that no hydrogenation had occurred. A mixture of 1: 1 ethanol · vinegar fe: and 3.0 grams of iron powder was added to the reaction mixture, and nitriding was continued for one hour at 65 ° C. Analysis of the reaction mixture then showed that hydrogenation was redundant. The reaction mixture was then cooled and filtered through celite. The filtrate was concentrated to a residue under reduced pressure. The residue was dissolved in dichloromethane 'and the solution was washed with water and then with an aqueous solution saturated with sodium carbonate. The organic layer was concentrated under reduced pressure to give 4 · 2 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step D as an intermediate {4-[(4- {bis [4- (trifluoromethyl) phenyl] methylene} hexahydropyridyl) methyl] phenyl} ethoxycarboxamide ( The synthesis of compound 5 5) in the table below will be 0.52 g (0.000 mol) in 5¾ liters of ethyl acetate 4_ [(4 _ {bis [(trifluoromethyl) phenyl]] Methylene} hexahydropyridyl) methyl] phenylamine with 0.20 g (0. 0020 mol) of the stirred solution of triethylamine was cooled to 0-5, and 0.11 g (0.010 mol) ethyl ethyl formate was added. When the addition is complete, the reaction mixture 90038-68-200427680 is stirred for about 10 minutes. The reaction mixture was then washed with a saturated solution saturated with potassium carbonate, and then concentrated to a residue under reduced pressure. The residue was purified by column chromatography on silica gel using a mixture of ethyl acetate and hexane as an eluent. The appropriate fractions were combined and concentrated under reduced pressure, yielding 0. 1 2 g of compound 144. The NMR spectrum is consistent with the proposed structure. Step E Synthesis of Compound 101 The solution of 0.06 g (0.00001 1 mole) of Compound 44 in 3 ml of methanol was stirred and added to 1. 5 ml of 30% hydrogen peroxide. At the end of the addition, the reaction mixture became cloudy and additional methanol was added to keep the reaction mixture clear. The reaction mixture was stirred at room temperature for about 3 days, during which time an additional 0.5 ml of 30% hydrogen peroxide was added to start the reaction to completion. The reaction mixture was then extracted with dichloromethane, and the extract was concentrated under reduced pressure to give 0.66 g of compound 101. The NMR spectrum is consistent with the proposed structure. Example 2 This example illustrates the preparation of N- (4-aminophenyl) ({苯基-[(4- (2-pyridyloxy) phenyl) methyl] (4-hexahydropyridyl)} [4 -(Trifluoromethyl) phenyl] methoxy) carboxamide (Compound 227 in the table below) Step A Synthesis of (4- (2-pyridyloxy) phenyl) methanol as intermediate 15.3 g (0.5 g) in 150 ml of methanol 077 mol) (4- (2-pyridyloxy) phenyl) formaldehyde (known compound), a stirred solution was cooled to 0-5 ° C, and 3. 2 grams (0. 085 mole) sodium hydride. At the end of the addition, the reaction mixture was allowed to warm to room temperature and stirred for 30 minutes. The reaction mixture was then cooled to 5 ° C and 150 ml of water was carefully added to destroy the excess borohydride 90038 -69- 200427680 sodium. The mixture was cooled to 0 ° C and neutralized with concentrated hydrochloric acid. Excess acid was added to make the mixture acidic. The mixture was made neutral by adding solid sodium bicarbonate. The mixture was concentrated under reduced pressure and some methanol was removed. The concentrate was dissolved in ethyl acetate and washed with an aqueous solution saturated with sodium vaporization. The organic layer was dried over sodium sulfate, filtered and concentrated under reduced pressure to yield 12. 6 grams of the title compound. The NMR spectrum is consistent with the proposed structure. Step B Synthesis of (4- (2-pyridyloxy) phenyl) methyl chloride as an intermediate will be 4.4 g (0.037 mole) of thionine in 75 ml of anhydrous digas methane. The stirred solution was cooled to 0 ° C and 0.07 g (catalyst) pyridine was added. Then dropwise add 5 in 25 ml of dichloromethane. 〇g (0. 025 mol) (4- (2-pyranyloxy) phenyl) methanol solution. At the end of the addition, the reaction mixture was allowed to warm to 22 ° C and stirred for 30 minutes. The entire reaction mixture was then dissolved in ethyl acetate and treated with solid sodium bicarbonate. The organic layer was dried over sodium sulfate, filtered and concentrated to a residue under reduced pressure. The NMR spectrum is consistent with the structure shown. Since the compound was unstable, the product was used without further purification. The estimated yield is about 5.0 grams. Step C Synthesis of 4- (trifluoromethylbenzylpyridylmethanol) as an intermediate. Carefully add 19 grams of 4-bromobenzotrifluoride solution in 62 ml of THF within 60 minutes. (0 079 mol) in a mixture of magnesium filings and iodine crystals (catalyst), while maintaining the reaction mixture at a temperature not exceeding 40 r .; After two, the reaction mixture is stirred and added dropwise to 45 ml of Ding $ 〇gram (0. 047 mole) solution of 4-pyridinecarboxaldehyde. When the addition is complete, the reaction mixture 90038-70-200427680 is stirred at room temperature for about 16 hours. The reaction mixture was then cooled to 0 C, and a sufficient amount of an aqueous solution saturated with ammonium chloride was added to stop the reaction. The mixture was then extracted with ethyl acetate, and the extract was washed with an aqueous solution saturated with sodium chloride. The extract was dried over sodium sulfate, filtered, and concentrated under reduced pressure to give about 15. 2 grams of crude product. Step D The synthesis of 4- (trifluoromethylphenyl) -4-hexahydropyridylmethanol hydrochloride as an intermediate will be 6. in 80 ml of ethyl acetate. 4 grams (0. 020 Mol) 4- (trifluoromethylphenyl) -4-pyridylmethanol solution was stirred, and anhydrous hydrogen chloride gas was bubbled through the solution, thus forming the hydrochloride of p-methyl alcohol intermediate . The salt was collected by filtration and washed with a small amount of ethyl acetate. The wet solid was then dissolved in 100 ml of ethanol and placed in a Parr hydrogenation bottle with 0.5 g (catalyst) platinum oxide. The mixture was then hydrogenated using a Parr hydrogenator at 45 pounds per square inch (psi) for about 75 minutes. The NMR obtained with the reaction mixture showed that the reaction was about 90% complete. Will be another 0. 25 grams of platinum oxide catalyst was added to the reaction mixture, and hydrogenation was continued for another 60 minutes at 45 psi. The reaction mixture was then filtered through diatomaceous earth. The mash was washed with digas methane, and the combined washings and the filtrate were concentrated under reduced pressure to give 5.2 g of the title compound. NMR light was consistent with the proposed structure. The reaction was repeated. Step E The synthesis of {1-[(4- (2-pyridyloxy) phenyl) methyl K4-hexahydropyridyl)} [4- (trifluoromethyl) phenyl] methanol as intermediate 6. in 31 ml DMSO 1 g (0. 021 mole) 4- (trifluoromethylphenyl) -4-hexahydropyridylmethanol hydrochloride solution was stirred and added to 1.0. 7 males 90038 -71-200427680 g (0. 083 mole) N, N-diisopropylethylamine. At the end of the addition, the reaction mixture was stirred for 10 minutes, and then 5. prepared in step 6 of this example was added. 〇 grams (0. 023 mole) (4- (2-pyridyloxy) phenyl) methyl chloride. At the end of the addition, the reaction mixture was stirred at ambient temperature for 16 hours. The reaction compound was then treated with aqueous 10% sodium carbonate and extracted with ethyl acetate. The ethyl acetate layer was washed with water, visually and then with an aqueous solution saturated with sodium vaporization. The ethyl acetate layer was dried over sodium sulfate, filtered, and concentrated under reduced pressure to a residue. The residue was purified by column chromatography on silica gel using a mixture of acetone and dichloromethane as an eluent. Combining the appropriate fractions and shrinking under reduced pressure yields 4. 2 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step F Synthesis of Compound 227 06 grams (0. 0004 mol) 4-chlorophenyl isocyanate sample was weighed and added to a two British coin vial ', then 1.2 ml of dichloromethane, 8 g (0. 0004 mol) {1-[(4- (2-pyridyloxy) phenyl) methyl] (cardiohexahydropyridyl)} [4- (trifluoromethyl) phenyl] methanol and 0.06 ml Triethylamine. The vial was tightly capped and gently shaken at 35 ° C for 16 hours using a vortex mixer. Dichloromethane was then removed under a stream of nitrogen to provide a residue. The residue was purified by column chromatography on silica gel using a mixture of acetone and methane as the eluent. Combining the appropriate collections and concentrating under reduced pressure yields 0. 2 g of compound 227. The NMR spectrum is consistent with the proposed structure. Example 3 This example is exemplified for the preparation of [(1-{[4- (2-methyl (1,2,3, 'tetracycline_5_yl)) phenyl] methyl} (4-hexahydropyridyl )) [4- (trifluoromethoxy) phenyl] methyl] 90038 -72- 200427680 Sample of propyl sulfonamide (Compound 433 in the table below) Step A as l- { The synthesis of [4- (2-methyl-1,2,3,4-tetrazol-5-yl) phenyl] T group} hexahydropyridine-4-carboxylic acid ethyl ester will be in 75 ml of DMSO and 99 30 in ml of methanol. 0 grams (0. 191 Mol) Stir the solution of ethyl isonapicate and add 61. 7 grams (0. 477 mole) N, N-diisopropylethylamine and then 40.2 g (0159 mole) 5- [4- (bromomethyl) phenylmethyl-; 1,2,3, 4-tetrazole (known compound-US 5,63 9,763). When the addition was complete, the reaction mixture was stirred at ambient temperature for about 72 hours. The reaction mixture was then diluted with 175 ml of ethyl acetate, and washed with a 175 ml solution of a saturated aqueous solution of sodium chloride and a portion of water. The organic layer was concentrated to a residue under reduced pressure. NMR analysis of the residue showed the presence of some of the raw material of isonapicate. The residue was dissolved in 370 ml of methanol and water was added to precipitate a solid substance. After standing for about 20 minutes, the solid was collected by filtration and washed with a cold solution of a portion of methanol and a portion of water. The solid was dried to give 32.9 g of the title compound. A second solid harvest was collected from the filtrate, yielding an additional 1.0 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step B The synthesis of 1-{[4- (2-methyl-1,2,3,4-tetrazol-5-yl) phenyl] methyl} hexahydro P as an intermediate 51 in 264 ml of THF. 6 grams (0. 1 57 mol) of a solution of 1- {〇 (2-methyl • 1,2,3,4-tetrazol-5-yl) phenyl] methyl} hexahydropyridine-4-carboxylic acid was stirred, And add 6 in 186 ml of water. 9 grams (0. 172 moles) of sodium hydroxide followed by 160 ml of methanol. When the addition was complete, the reaction mixture was stirred at ambient temperature for 2 hours. The reaction mixture was then concentrated under reduced pressure to a residual 90038-73-200427680. The residue was dissolved in 250 ml of water and the solution was cooled to about 4t. The falling liquid was then neutralized with concentrated hydrochloric acid to give a solid. Under nitrogen flow, water was removed within about 60 hours. The resulting solid was dried in a vacuum oven to give 53. 4 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step C as an intermediate 丨-{[4- (2-methyl (1 and 3, tetrazol-5-yl is phenyl) methyl} (4-hexahydropyridylmethoxymethyl complex) The synthesis of amine will be 47.7% in 675 ml. 2 grams (〇. 157 mole) 1-{[4- (2-methyl 1,2,3,4-tetrat-5-yl) phenyl] methyl} hexahydropyridinecarboxylic acid solution was stirred and added 18. 3 grams (0. 1.88 mole) N, 0-dimethylhydroxylamine hydrochloride. The reaction mixture was cooled to 0 ° C and added to 3.0. 7 grams (0. 188 mole) diethyl cyanophosphonate and then 34.9 grams (0. 345 moles) triethylamine. At the end of the addition, the reaction mixture was allowed to warm to ambient temperature and stirred for 2 hours. The reaction mixture was then diluted with ethyl acetate and a water solution saturated with sodium chloride and water. The aqueous layer was separated from the organic layer and washed with ethyl acetate. The washing liquid was then combined with the organic layer, and the combined product was washed with one part of water and then four parts of 150 liters of a saturated aqueous solution of sodium chloride. The mixture was dried over sodium sulfate 'filtered and concentrated under reduced pressure to give 44.1 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step D 1-{[4- (2-methyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl} (4-hexahydropyridyl) as an intermediate 4. · Synthesis of (trifluoromethoxy) phenyl ketone: 44.1 g (0.128 mol) ΐ-{[4- (2-methyl (1,2,3,4) in 65 ml of THF -Tetramethyl-5 -yl)) phenyl] methyl} (4-hexahydro-p-r-methyl) -N-methoxy 90038 -74- 200427680 -N-f-carboxamide solution was added in 133 ml tHF is a Grignard reagent prepared by 46. 2 grams (0.192 mole bromotrifluoromethoxybenzene and 50 grams (0205 grams_atoms) of metal). The reaction mixture was warmed to 60 ° C, and it was stirred for another 60 minutes. Then the reaction mixture was poured into 101. 15.5 ml of a cold solution of concentrated hydrogen acid in 5 ml of ethanol 'and stirred for 5 minutes. The mixture was diluted with dichloromethane and washed with an aqueous solution saturated with sodium bicarbonate. The organic layer was washed with a saturated aqueous solution of sodium chloride 'and dried over sodium sulfate and filtered. The filtrate was concentrated to a residue under reduced pressure to give 58. 5 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step E (Hydroxyimino) as intermediate (中间-[[4- (2-methyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl]) (4 -Hexargyridine) Synthesis of [4- (trifluoromethoxy) phenyl] methane will be 40% in 641 ml of ethanol. 〇g (0. 090 mole) 1 _ {[4- (2-methyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl} (4-hexahydropyridyl) 4- (trifluoro Aqueous (oxy) phenyl ketone solution was stirred and added 6. 3 grams (0. 091 mole) Hydroxylamine Hydrogenate and then add 9. 1 g (0. 090 mole) triethylamine. At the end of the addition, the reaction mixture was warmed to reflux and stirred for 16 hours. Then another 0.1 equivalents of hydroxylamine hydrochloride and triethylamine were each added to the reaction mixture, and heating was continued under reflux for another 3 hours. The reaction mixture was then cooled and concentrated to a residue under reduced pressure. The residue was dissolved in dichloromethane, and washed successively with an aqueous solution saturated with sodium bicarbonate and an aqueous solution saturated with sodium chloride. The organic layer was concentrated to a residue under reduced pressure. The residue was dried under reduced pressure to yield 39. 9 g of the title compound. The NMR spectrum is consistent with the proposed structure 90038 -75-200427680. Step F ^ [4- (2-methyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl] (4-hexahydropyridyl) [4 · ( The synthesis of trifluoromethoxy) phenyl] methylamine will be 39. in 100 ml of THF. 9 grams (0. 087 mole) (#i 基 imido) (1-[[4- (2-methyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl]) (4 -Hexahydropyridyl) [4- (trifluoromethoxy) phenyl] methane stirred solution was cooled to -10〇 :, and added 19. 1 ml (0. 191 mol-1 g molecular weight in THF) lithium hydride. At the end of the addition ', the reaction mixture was warmed to 65 ° C and allowed to stand for 25 hours. The reaction mixture was then cooled to about ambient temperature and added via cannula to a cooled, stirred aqueous solution saturated with ammonium chloride. The mixture was then extracted with ethyl acetate and the extract was cannulated from the aqueous layer. The combined extracts were concentrated to a residue under reduced pressure. The residue was dried to give 361 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step G Synthesis of Compound 433 will be 0. 30 grams (0. 0007mol) 1-[[4- (2-methyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl] (4-hexahydropyridyl) [4- (tri Fluoromethoxy) phenyl] methylamine, 0. 10 grams (0. 0007mol) 丨 _ propanesulfonium gas and 0. 11 grams (0. 0011 mole) triethylamine solution was stirred at ambient temperature for about 18 hours. The reaction mixture was then concentrated to a residue under reduced pressure. The residue was purified by column chromatography on silica gel using hexane, ethyl acetate, and mixtures thereof as eluents. The appropriate fractions were combined and concentrated under reduced pressure to yield 0.07 g of compound 433. The NMR spectrum is consistent with the proposed structure. 90038 -76- 200427680 Example 4 This + example is exemplified for the preparation of 2 _ [(1 _ {[4_ (2_methyl〇, 2,3,4_tetracycline_5_yl)) dong] methyl} (4 -Hexyl chloride)) [4_ (trifluoromethoxy) phenyl] methoxy] quino- (trifluoromethyl) pyridine (Compound 434 in the table below) Step A # is the intermediate Synthetic effect of 4- "yl 4- (trifluoromethoxy) phenylphosphonium", a solution of gram (0.0 · mol) 4-cyanopyridine in 50 ml of THF was added to 21. 3 grams (0. 088 mole) 1-bromo-4 · trifluoromethoxybenzene and 2. 5 a gram (0. In the Grignard reagent prepared by 102 g-atomic) magnesium metal. When the addition was complete, the reaction mixture was stirred at 4 ° C for 8 hours. The reaction mixture was then poured into a dilute aqueous solution of ammonium chloride and acidified to pH 3 with 10% aqueous hydrochloric acid. Dichloromethane was extracted and the combined extracts were dried over sodium sulfate. The mixture was filtered and the filtrate was concentrated to a residue under reduced pressure. The residue was subjected to acetone, dichloromethane and mixtures as eluents. The silica gel was purified by column chromatography. The appropriate fractions were combined and concentrated under reduced pressure to give the title compound. The NMR spectrum was consistent with the proposed fiber structure. Step B 4-pyridyl 4- as an intermediate The synthesis of (trifluoromethoxy) phenyl ketone hydrochloride will be 20% in 350 ml of ethanol. A solution of 0 g (0.075 mole) of 4-pyridyl 4- (difluoromethoxy) phenyl ketone was stirred, and hydrogen chloride gas was bubbled through for 5 minutes. At the end of the addition, the reaction mixture was stirred for 1 h and then it was filtered to collect a solid. The solid was washed with three portions of diethyl ether and dried in a vacuum oven, yielding about 22. 0 g of the title compound. The NMR spectrum is consistent with the structure proposed by 90038-77-200427680. Step C Synthesis of 4-hexahydropyridyl [4- (trifluoromethoxy) phenyl] methanol hydrochloride as an intermediate 1. 0 g (catalyst) platinum oxide was added to a 2000 ml Parr hydrogenation bottle, and the hydrogenation bottle was flushed with anhydrous nitrogen. Then move 1. 0 grams of platinum oxide and 22.50 in 75 ml of ethanol 0 g (0.072 mol) of 4- (trifluoromethoxy) phenyl ketone hydrogen rat salt) was added to the bottle. Place the bottle in a Parr hydrogenator and subject the inner grains in the bottle to hydrogenation conditions. When the theoretical amount of hydrogen has been absorbed, 'the bottle is taken out of the hydrogenator and the contents are passed through the celite. The filter block was washed with monochloromethane, and the combined filtrate and washings were concentrated under reduced pressure 'to give the title compound. The NMR spectrum is consistent with the proposed structure. Step D {1-[(2-methyl (1,2,3,4-tetrazol-5-yl)) methyl] (4-hexahydropyridyl)} [4- (trifluoro The synthesis of methoxy) phenyl] methanol was carried out in a manner similar to Step E of Example 3, using 7. 0 grams (0. 026 mole) 4-hexahydropyridyl [4- (trifluoromethoxy) phenyl] methanol hydrochloride, 6-8 grams (0. 026 mole) 5- [4- (bromomethyl) phenyl] _2-methyl-1,2,3,4-tetrazole (prepared in a manner similar to step A_c of Example 4) and 9 . 9 grams (0. 077 mole) N, N-diisopropylethylamine to prepare the compound. The NMR spectrum is consistent with the proposed structure. Step E Synthesis of Compound 434 will be 0. 0 in about 10 ml of DMSO. 89 g (0.02 mol) {丨-[(2-methyl (1,2,3,4-tetrazol-5-yl)) methyl] (4-hexahydropyridyl)} [ 4-gas trifluoromethoxy) benzyl] methanol, 0. 36 grams (0. 002 mole) 2-fluoro-5-trifluoromethylpyridine 90038 -78- 200427680 and 0. 08 grams (0. 002 mol) of 60% hydrogenate was heated at 85-9 (TC for 3 hours with sodium chloride (in mineral oil) and stirred and then allowed the reaction mixture to cool to ambient / dish degree 'and then poured into water. The mixture was extracted with diacetic acid and the extracted extract was dried over magnesium shiwamate. The mixture was filtered and the filtrate was reduced to a residue under reduced pressure. The residue was dried using dichloromethane and methanol ( The mixture was used as an eluent for gelatin purification by f-column chromatography. The appropriate fractions were combined and concentrated under reduced pressure to yield 0. 63 g of compound 434. The NMR spectrum is consistent with the proposed structure. Example 5 A remote example is exemplified for the preparation of (3,5_difluorophenyl ^ {丨 heptapyrimidine 2-oxyphenyl) methyl] (4-1,2,5,6-tetrahydropyridine Group)} [4- (trifluoromethyl) phenyl] methoxy) carboxamide (compound 786 in the table below) Step A 2- [4- (chloromethyl) phenoxy as intermediate Synthesis of Pyridyl] pyrimidine: 40 g (002 mol) (4-pyrimidine_2-oxyphenyl) fluorenol (known compound) and 7 drops of pyridine The stirred solution was cooled in an ice-water bath and added dropwise 2. 〇mL (0. 027 mole) solution of thionine chloride. At the end of the addition, the reaction mixture was stirred at about 10 ° to 20 ° C for 3 hours. The reaction mixture was then poured into a cold aqueous sodium bicarbonate solution. The mixture was then stirred for 30 minutes and the organic layer was separated. The aqueous layer was extracted with a 50 ml portion of dichloromethane. The extract was combined with the organic layer, and the combination was passed through a silicone-coated filter paper to remove a small amount of water. The filtrate was concentrated under reduced pressure to give □ g of the title compound. The NMR spectrum agrees with the proposed structure. 90038 -79- 200427680 Synthesis of ‘pyridyl [4- (trifluoromethyl) phenyl] methanol as an intermediate Under normal water and nitrogen, an appropriate amount of freshly cut magnesium flakes was suspended in 15 ml of THF. A solution of 225 grams (0.01 mole) of 'bromobenzodifluoride in 5% in 75 ml of THF was added thereto. The reaction mixture was then warmed to about 30 ° C to begin the reaction. Once the reaction has proceeded, the temperature of the reaction mixture was maintained at about 34 within 1 hour. (: Add the remaining 4-bromobenzodifluoride solution to a rate of about 38 ° C. When the addition is complete, stir the reaction mixture for one hour, cool it to ambient temperature. Then add in 75 ml THF in portions. Of 8. 5 g (0. 075 mole) solution of 4-pyridylcarboxaldehyde while maintaining the temperature of the reaction mixture below 30 ° C. When the addition was complete, the reaction mixture was stirred at ambient temperature for about 18 hours. The reaction mixture was then poured into 600 * liters of 10% aqueous ammonium gaseous agitation with vigorous stirring. The mixture was extracted with 300 ml portions of ethyl acetate. The combined extracts were washed with 250 ml of a saturated aqueous solution of sodium chloride, and then dried over magnesium sulfate. The mixture was filtered and the filtrate was concentrated under reduced pressure to yield 21. 2 g of the title compound. This product was used in the following reaction without purification. Step C Synthesis of 4-pyridyl [4- (trifluoromethyl) phenyl] methanol hydrochloride as an intermediate 2 grams (0. 070 mol) 4-pyridyl [4- (trifluoromethyl) phenyl] methanol solution was stirred vigorously, and anhydrous hydrogenated gas was added below the surface of the solution within 15 minutes. The reaction mixture was then stirred for an additional 15 minutes, and the solid was collected by filtration. The solid was washed with ethyl acetate and dried to yield 11. 4 g of the title compound. NMR spectrum and proposed structure 90038 -80- 200427680 — cause 〇 Step D as φ μ 1, 1, 3, U-[(4-pyrimidine-2-oxyphenyl) methyl] (4-pyridine )} Synthesis of [4- (trifluoromethyl) phenyl] methanol hydrochloride Υ〆Αg (0.011 mol) whole 4-pyridyl [4- (trifluoromethyl) benzene Methyl] -prehydrochloride is separated between diethyl ether and aqueous sodium bicarbonate solution. The ether layer was opened and dried over magnesium shiwanate. The mixture was filtered and the filtrate was filtered under reduced pressure to a residue. The residue was dissolved in 100 ml of acetone, and A g (0. 0113 mole) 2_ [4- (chloromethyl) phenoxy] pyrimidine and 0.2 g (0. 0012 mole) potassium iodide. When the addition was complete, the reaction mixture was warmed to π C and stirred for about 8 hours. The reaction mixture was then concentrated under reduced pressure to a residue, and the residue was triturated with 150 ml of diethyl ether to give 5.2 g of a solid product when dried. The NMR spectrum is consistent with the proposed structure. Step 骡 E as the intermediate {1-[(4-pyrimidin-2-oxyphenyl) methyl] (4-1,2,5,6-tetrahydropyridyl)} [4- (trifluoromethyl (Phenyl) phenyl] methanol Synthesis of ι · 〇g (0.002 mol) {1-[(4-pyranyloxyphenyl) methyl] (4-pyridyl) in 30 ml ethanol } Tax storage of [4- (trifluoromethyl) phenyl] methanol hydrochloride> Cereals are cooled in an ice-water bath 'and a portion of 0. 1 g (0.0026 mol) of sodium borohydride. At the end of the addition, the reaction mixture was at about 10%. Stir at 0 to 20 ° C for 3 hours. The reaction mixture was then diluted with 100 ml of water and extracted with two 75 ml portions of ethyl picrate. The combined extracts were washed with 75 ml portions of 10% aqueous lithium chloride, and the combination was dried over sodium sulfate. The mixture was then filtered and the filtrate was concentrated to a residue under reduced pressure. The residue was purified by column chromatography on 90038-81 &quot; 200427680 using a 1% to 2% methanol / digas methane mixture as the eluent neutral oxidant (6X) water. Appropriate collections were combined and under reduced pressure: 纟 辰 纟 伴 'to produce 0.44 g of the title compound. The n M R spectrum is consistent with the proposed structure. Step F Synthesis of Compound 7 8 6 In a manner similar to Step F of Example 2, a 0. 15 in 15 ml of dichloromethane was used. 44 grams (0. 0010 mole) {丨-[(4-pyrimidin-2-oxyphenyl) methyl] (4-1,2,5,6-tetrahydropyridyl)} [4- (trifluoromethyl) benzene Methyl] methanol, 0.2 g (0.2 g) 0014 mole) 3,5-difluorophenyl isocyanate '〇 · ΐ 4 g (0. 0014 mole) triethylamine and 0. 05 g (catalyst) of 4-dimethylaminopyridine was used to prepare the compound. The reaction product was purified by column chromatography on column gels using 10 to 25% of an acetone / dichloromethane mixture as an eluent. The appropriate fractions were combined and concentrated under reduced pressure to yield 0.18 g of compound 7 8 6 with a melting point of 85-92 ° C. The NMR spectrum is consistent with the proposed structure. Example 6 ^ Haibei example is used to prepare N-(4-chlorophenyl) ({1-[(4-(2 ^ than dianoxy) phenyl) methyl] (4- (1-oxy Hexahydropyridyl)))} [4- (trifluoromethyl) phenyl] methoxy) carboxamide (compound 395 in the table below) will be 12. 9 grams (0. 0216 Mol) Compound 227 (prepared by the method of Example 2) and a solution of 390 grams of methanol were stirred, and 1177 grams (丨. 7315 moles) of 50% aqueous hydrogen peroxide. At the end of the addition, the reaction mixture was stirred for 48 hours while monitoring the completion of the reaction by high pressure liquid chromatography and nmR analysis. The reaction mixture was then concentrated under reduced pressure, methanol was removed, and the concentrate was then extracted with dichloromethane. Dichloromethane was removed under reduced pressure and 90038 -82- 200427680 left a residue. The residue was purified by column chromatography on a neutral oxide (6% water) using a methanol / dichloromethane mixture of 6% to 2% as the eluent. The appropriate fractions were combined and concentrated under reduced pressure to yield 9. 2 g of compound 395. The NMR spectrum is consistent with the proposed structure. Example 7 This example exemplifies the preparation of N_ (4_chlorophenyl) ({ι_ethoxy-WM2-eryloxy) phenyl) fluorenyl] (4_hexaaminop than fluorenyl)} ㈣ Three gas methyl) phenyl] methoxy) chloramine amine ethyl phosphonium salt (&amp; compounds in the table below a sample will be 0.5 grams (0 · 8 moles) of compound in 10 ml of chloroform 493 (made in Example 6) w. The solution of 25 g (0-6 mol) of diethyl sulfate was heated under reflux for 24 hours. The reaction mixture was then concentrated under reduced pressure to a residue. The residue may be washed with triethyl ether and washed with diethyl ether. The residue was dried at room temperature to give 0.57 g of a solid material. Dissolve the solids in chloroform and pre-sink the house with ml of diacetic acid. The gas was decanted and the residual solid was dried under reduced pressure to yield 0.45 g of compound 86. The NMR spectrum is consistent with the proposed structure. Example 8 [4- (trifluoromethyl) phenyl] imidine (compounds in the table below. This example is exemplified for the preparation of 2-{'[[bismethyl} hexahydropyridyl] methyl} phenoxy } Nan824) The sample was 3m + A similar to step B of Example 1, using 26 in 200 g of DMF. 0 g (0.110 mol) 孓 [heart (air-based) winter oxy] pyrimidine hydrochloride (made in a manner similar to that of step A of Example 7) (αα, 士, 所), 34. 0 grams (0. 088: 90038 -83-200427680 Mol M- {bis [4- (trifluoromethyl) phenyl] methylene} hexahydropyridine (prepared in Step A of Example 2), 36. 0 grams (0. 2604 mol) carbonic acid, but the compound is prepared. Yield of compound 824 is 41. 0 grams. The NMR spectrum is consistent with the proposed structure. Example 9 This example exemplifies the preparation of 2_ {4-[{bis [4- (trifluoromethyl) phenyl] fluorenyl} 丨-(oxyhexahydropyridyl) methyl] phenoxy} pyrimidine (Compound 854 in the table below) The sample was used in a manner similar to Step E of Example 1, using 40.40 in 140 ml of methanol. This compound was prepared from 0 gram (0.007 mol) of compound 824 (prepared in Example 8) and 50 grams of 30% hydrogen peroxide. The yield of compound 854 is 35. 〇 grams. The NMR spectrum is consistent with the proposed structure. Example 10 This example illustrates the preparation of 2- {4-[(9-aza-3- {bis [4- (trifluoromethyl) fluorenyl] methylene]} bicyclo [3. 3. 1] Non-9-yl) methyl] phenoxy} P sample (Compound 117 in the table below) In a manner similar to Step A of Example 1, 0. 0 in trifluoroacetic acid was used. 1 8 grams (0. 00025 mole) {9-aza-9-[(4- (2-pyridyloxy) phenyl) methyl] bicyclo [3. 3. 1] Non-3-yl} bis [4- (trifluoromethyl) phenyl] methanol (known compound disclosed in U.S. Statutory Invention Registration H1,838) to prepare the compound to give compound 117. The NMR spectrum is consistent with the proposed structure. Example Π This example exemplifies the preparation of 1-[(1-[[4- (2_ethyl (1,2,3, cardiotetrazolidine-yl)) phenyl] methyl] (4-hexahydro Pyridinyl))) [4- (trifluoromethyloxy) phenyl] methyl 90038 -84-200427680 oxy] -4- (trifluoromethoxy) benzene (Compound 137 in the table below) Step A As an intermediate, 5- (4-methylphenyl)-丨, 2,3,4-tetrazole will be synthesized in 160 ml of DMF 10. 0 grams (0. 085 mol) Stir the solution of -Nitrile and add 5. 6 grams (0. 085 mole) sodium azide. At the end of the addition, the reaction mixture was warmed to 135 ° C and stirred for 3 hours. The reaction mixture was then cooled and poured into 200 ml of stirred 1 eq of cold aqueous hydrogen acid. At the end of the addition 'the mixture was stirred for 5 minutes and filtered to collect a white solid. The solid was dried in a vacuum oven at 35-40 ° C for 16 hours, yielding 7. 丨 grams of the title compound. The reaction was repeated. Step B Synthesis of 2-Ethyl-5- (4-methylphenyl) as an intermediate 0 grams (0. 125 mol) 5- (4-methylphenyl) -1,2,3,4-tetrazole solution was stirred and added 48. 7 grams (0. 312 Mol) Kiki Aceto and then join 17. 3 grams (0. 125 moles) potassium carbonate. At the end of the addition, the reaction mixture was warmed to reflux and stirred for 2 hours. The reaction mixture was then concentrated to a residue under reduced pressure. The residue was dissolved in ethyl acetate and filtered. The filtrate was concentrated to a residue under reduced pressure. The residue was purified by column chromatography on silica gel using 1: 4 ethyl acetate · hexane as an eluent. Combining the appropriate collections and concentrating under reduced pressure yields 18. 8 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step C The synthesis of 5- [4- (bromomethyl) phenyl] ethyl 1,2,3,4-tetramidine as an intermediate will be in 156 ml of carbon tetrachloride 18. 8 grams (0. 100 mol) 2-ethyl 90038 -85-200427680 _5- (4-methylphenyl) -1,2,3,4-tetra wah solution was stirred and added 19. 6 g (0. 110 mol) N-bromosuccinimide, followed by 0.24 g (o. ool)) benzene peroxide. At the end of the addition, the reaction mixture was heated to reflux and stirred for 90 minutes. The reaction mixture was then cooled and filtered. The filtrate was concentrated under reduced pressure to yield 27. 7 g of the title compound. The NMR spectrum is consistent with the structure that has just been elucidated. Step D As the intermediate, 1-{[4- (2-ethyl-1,2,3,4-tetrazol-5-yl) phenyl] methyl} hexahydropyridine-4-carboxylic acid ethyl ester The synthesis will be 16.0 g (0.5 g) in 50 ml of DMSO and 66 ml of methanol. 102 mol) Stir the solution of ethyl isonic acid and add 44 ml (0. 256 moles) N, N-diisopropylethylamine and then added 22. 8 grams (0. 085 mol) 5- [4-(/ Omethyl) benzyl] -2-ethyl-1,2,3,4-tetrafluorene. When the addition is complete, stir the reaction mixture at ambient temperature; stir for about 72 hours. The reaction mixture was then diluted with 130 ml of ethyl acetate and washed with a 1: 1 saturated aqueous solution of sodium chloride and water. The organic layer was washed with a saturated aqueous solution of sodium chloride and water, dried over sodium sulfate and filtered. The filtrate was concentrated to a residue under reduced pressure. The residue was purified by column chromatography on silica gel using a mixture of dichloromethane and acetone. Combining the appropriate fractions and condensing under reduced pressure 'yields 20. 9 g of the title compound. NMR spectroscopy and proposed structure—Caution 0 Step E as 1-{[4- (2-ethyl-1,2,3,4-tetrafluoren-5-yl) phenyl] methyl} hexa The synthesis of hydrogen p-dopedioic acid will be 20 in 132 ml of THF. 9 grams (0. 078 molar core (2ethyl-1,2,3,4-tetrazol-5-yl) phenyl] methyl} hexahydropyridine-4-carboxylic acid ethyl acetate solution 90038 -86- 200427680 Then, 3.4 g (0.086 mol) of sodium oxide in 93 升 liter of water was added, followed by 80 liters of nail polish. At the end of the addition, the reaction mixture was allowed to stir for 2 hours at ambient agitation. The reaction mixture was then concentrated to a residue under reduced pressure. The residue was dissolved in toluene and concentrated under reduced pressure to remove any remaining solvents. The residue was dissolved in 100 ml of water and extracted with diethyl ether. The aqueous layer was cooled to about 100%, and ρ7 was reached with concentrated hydrochloric acid. The resulting solid was collected by filtration, washed with water and dried to give 18.2 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step F as 1-{[4- (2-ethyl (1,2,3,4-tetrazol-5-yl)) phenyl] methyl} (4-hexahydropyridyl) methoxy Synthetic effect of methylmethylchitamic acid amine will be 18.2 g (0.1 g) in 240 ml of DMF. 058 Mol) 1-{[4- (2-ethyl 1,2,3,4-tetrazol-5-yl) phenyl] methyl} hexahydropyridinecarboxylic acid solution was stirred and added 6. 8 grams (0. 070 mole) N, 0-dimethylhydroxylamine hydrochloride. The reaction mixture was cooled to 0 ° C. and 11.1 was added. 3 g (0.07 mole) monoethyl cyanophosphonate, followed by 17. 8 ml (.27 mol) of triethylamine. At the end of the addition ', the reaction mixture was stirred for 2 hours, and then it was diluted with ethyl picoate and a 1: 1 saturated aqueous solution of sodium chloride and water. To help separate the organic layer from the aqueous layer ', hexane and solid sodium chloride were added to the reaction mixture. The organic layer was separated and washed with water and then with an aqueous solution saturated with sodium chloride. The mixture was dried over sodium sulfate, filtered and concentrated under reduced pressure to yield 18. 5 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step 骡 G as 1-{[4- (2-ethyl (丨, 2,3,4-tetrazol-5-yl)) phenyl] methyl} (4-hexahydro p ) 4- (trifluoromethoxy) phenyl 90038 -87- 200427680 The synthesis of ketone will be 9 in 13 ml of THF. 3 grams (0. 026 mole) l-{[4- (2-ethyl (1,2,3, cardiotetramethyl)) phenyl] methyl} (4-hexahydropyridyl) -N-methoxy-N -A solution of methyl # transg-monamine was added in 27 ml of THF to 9.3 g (0.039 mols. 4 *) trifluoromethoxybenzene and 1. 0 grams (0. 041 grams-atomic) magnesium Grignard reagent. When the addition was complete, the reaction mixture was allowed to stand at ambient temperature for 90 minutes, and then warmed to Sichuan ", and stirred for an additional 60 minutes. Then the reaction mixture was poured into 13 ml of concentrated chloroacid in 93 ml ethanol The solution was stirred in the cold solution for 10 minutes. The mixture was diluted with dichloromethane and washed with a dilute aqueous solution of sodium bicarbonate. The organic layer was dried over sodium sulfate and filtered. The filtrate was concentrated to a residue under reduced pressure. Thing, yielding 10. 2 g of the title compound. The NMR spectrum is consistent with the proposed structure. Step Η {4- [Chloro (ΐ-{[4- (2-ethyl (1,2,3,4-tetratyl)) phenyl] methyl} (4-hexahydropyridine as intermediate Group) Synthesis of methyl] phenoxy} trifluoromethane will be 1-{[4- (2-ethyl (fluorene, 2,3,4-tetrazol-5-yl) in diethyl ether) ) Phenyl] methyl} (4-hexahydrohydrocarbyl) 4- (trifluoromethoxy) phenyl ketone and phosphorous chloride solution was heated under reflux for about 2 hours. The reaction mixture was then concentrated under reduced pressure to give the title compound. Step I Synthesis of compound 13 7 will be {4- [chloro group (1-{[4- (2-ethyl (ι, 2,3,4-tetrazol-5-yl)) phenyl in DMF A solution of] methyl} (4-hexahydropyridyl)) methyl] phenoxy} trifluoromethane, 4- (mainfluorofluorenyloxy) phenol and potassium carbonate was stirred at ambient temperature for about 2 hours. The reaction mixture was then poured into water, and the mixture was taken as ethyl acetate 90038 -88- 200427680. The extract was dried over magnesium sulfate and filtered. The filtrate was concentrated under reduced pressure to give compound 1 37. Those of ordinary skill in the art will recognize that compounds of the formula of the invention may include optically active and racemic forms. Compounds also known in the art as compounds of formula I may include stereoisomeric forms, tautomeric forms, and / or exhibit polymorphs. The invention naturally includes any racemic, optically active, polymorphic, tautomeric or stereoisomeric form or mixtures thereof. It should be noted that it is well known in the art how to prepare optically active forms, such as the disassembly of racemic mixtures or the synthesis of optically active intermediates. Some additional examples of compounds useful in the present invention are set out in the following table: Table 1 N-substituted (substituted arylmethyl) hexahydropyridines and p-pyridines with insecticidal properties

What is the formula I &amp; A in which A is C and forms hexahydro? Specific ring; m, p, q, recognition system 0; continued, 0 '1 90038 -89- 200427680 bond formed between the 4_ position of the fluorene-based carbofluorene and the hexahydrocarbon ring; R10, RM, Ri2 and R13 substituted phenyl groups; of which R2, R5, R6, R9, R1G, R12 and R13 are hydrogen:

Compound number R3 R4 R8 Rii 1 Η Η HH 21 Η Η HH 34 Η Η HH 41 Cl Η HH 51 Η C1 HH 61 F Η HH 76 Η FHF 8 Η cf3 H cf3 9 Η 〇cf3 H 〇cf3 10 Η c2h5 H c2h5 11 Η Cl ch3 H 12 Η cff3 ch3 ocf3 A compound of formula I, in which A is C and forms a hexahydro p ratio ring; m, p, q and r are 0; s is 1; n is 0, at methyl carbon (A) Forms 90038 -90- 200427680 with the 4-position of the hexahydropyridine ring

90038 -91-200427680 18 I Yiyi 20 21 22 23 24 I 25 26 27

CF3 H Η H Π H ffi H H ffi H000¾ K a K K E E

03¾03¾ 04¾ 04¾CH002H4cno) C3H6CIT0) PHSNHClro) 04H8NHCH0) clrs) NH

17 H F 16

15E

14 H F (0R2R ^) x- (0RSRS) y

F ffi

ι 3 H C7K β (CRjR ^ xCRSRS) y (CR ^ RJ ^ ACRSR ^

(CRjR ^ ACRgRSY

Hmm KH Ktmm i H 4 ^ 3 丨 驷 E ffi21 ^^^-lv -— ^^ #-4-1 · 3-H ^ H 7- ^ w &gt; 14- ^ 4b · lv ^ i4 ^^ ffi 【3 , 2-3.]. Hang on disease, 5-1-6- ^ ffi 7- f if ^ play this H 〔3,2-3,〕 ^ ill — 1,2,3V 丨 SA,? R &amp; 丨-丨 M Mountain 2 —— do if [0] sound meal contest 1,3-Bu Feng-2 丨 fresh — for H 1 丨 ^ &gt; 丨 — 丨 oc (offi3) 3 ί on (offi3) 3 — 2-(^. ^-3-^)-^-^^ i 2- (2- f 驷 Wu Weishen; &amp;! — OH- H CS5 KH Η FanffiF CF3 H ffi ffi ffi KH ffi so® Η K ffi ffi

E

x 3¾ y RS / RS κ

Rs R 2 90038 -92-200427680 Compounds of formula I, where A is C and forms a hexahydropyridine ring; m, p, q and r are 0; s is 1; η is 0, at methyl carbon (a) and six A double bond is formed between the 4-positions of the hydrogen p ratio ring; E series- (CR27R28) x- (CR29R30) y (unless otherwise specified) (where X series 1 and y series 0); R8 series uses R22 , R23, R24, R25, and R26; B is a phenyl substituted with R9, R1Q, R11, R12, and R13; of which R2, R5, R6, R9, R12, R13, R25, R26, R27, and R28 System hydrogen; R24

I Compound number r3 / r4 R22 R23 R24 Rl0 / Rn 28 H / F Η Η Η Η Cl 29 H / F Η Η Η Η F 30 h / cf3 Η Η Η Η Η 31 h / cf3 Η Η Η Η F 32 H / OCF3 Η Η Η Η 33 H / CF3 Η Br Br 90038-93-200427680 Compound No. r3 / r4 R22 R23 R24 R10 / R11 cf3 34 h / cf3 HHFHH 35 H / OCF3 HHFHH 36 Η / Cl HFFHH 37 H / FHFFHH 38 H / CF3 HFFHH 39 H / Cl HH OCH3 HH 40 H / FHH OCH3 HH 41 H / CF3 HH OCH3 HH 42 H / OCF3 HH OCH3 H OCF3 43 h / c2h5 HH OCH3 H C2H5 44 H / OH HH OC3H7 H OH 45 CF3 / HHH oc3h7 cf3 H 46 H / CF3 HH 〇c3h7 H cf3 47 OCF3 / HH 〇c3h7 OCF3 H 48 H / OCF3 HH oc3h7 H OCF3 49 H / OCF3 OCH3 H 〇c3h7 H 〇cf3 90038 -94- 200427680 r3 / r4 R22 R23 R24 Rio / R1 50 h / cf3 HH c〇2c2h5 Η cf3 51 h / cf3 HH C02CH (CH3) 2 Η cf3 52 h / cf3 HH NHC (= 0) CH3 Η cf3 53 h / cf3 HH NHC (= 0) CF3 Η cf3 54 h / cf3 HH NHC02CH3 Η cf3 55 h / cf3 HH NHC02C2H5 Η cf3 56 h / cf3 HH n (ch3) co2c2h5 Η cf3 57 h / cf3 HH NHC02C3H7 Η cf3 58 h / cf3 HH NHC02CH (CH3) 2 Η cf3 59 h / cf3 HH nhco2ch2 ch (ch3) h / cf3 HH ch = n〇c2h5 Η cf3 61 h / cf3 HH 1,3-thiazol-2-ylmethoxyΗ cf3 62 h / cf3 HH p ratio lake 2-ylΗ cf3 63 h / cf3 HH 3 -Chloropyridin-2-ylsulfonium cf3 64 h / ocf3 HH 3-chloropyridin-2-ylsulfonium 〇CF 65 H / CF3 HH 5-muryl ^ 7 specific disease-2-ylsulfonium cf3 66 H / CF3 HH 6-Ranyl p-pyridine-2-ylpyrene 90038 -95-200427680 Compound No. r3 / r4 R22 R23 R24 R10 / R5 67 h / cf3 HH 3-Dimuryl p-pyridine-2-yl cf3 Η 68 h / ocf3 HH 3-trifluoromethyl p-pyridin-2-yl cf3 Η 69 H / CF3 HH 5-dimuryl p-pyridin-2-yl OCF: Η 70 H / CF3 HH 3-cyanopyridine 2-yl cf3 Η 71 H / CF3 HH 5-cyanopyridine-2-yl cf3 Η 72 H / CF3 HH 3-nitrop ratio yodo-2-yl cf3 Η 73 H / CF3 HH 3- (methoxy Carbonylamino) -pyridin-2-ylcf3 Η 74 H / CF3 HH 2-methyl-2H-tetrazol-5-yl cf3 Η 75 H / CF3 HH 2-methyl-2H-tetrazole-5- Cl Η 76 Η / Cl HH 2-ethyl-2H-tetrazol-5-yl cf3 Η 77 Η / Cl HH 2-ethyl-2H-tetrazol-5-ylfluorene Η 78 H / FHH 2-ethyl-2H-tetrazol-5-ylCl Η 79 H / FHH 2-ethyl-2H-tetrazole-5 -Yl F Η 80 H / CF3 HH 2-ethyl-2H-tetrazol-5-yl C1 Η 81 H / CF3 HH 2-ethyl-2H-tetrazol-5-ylΗ Η 82 H / CF3 HH 2 -Ethyl-2H-tetrazol-5-yl F Η 90038 -96 cf3 200427680 R10 / Rn compound R3 / p4 r22 r23 number 2-ethyl-2H-tetrazo-5-yl ocf2〇-

84 H / H ch3 Cl H 85 H / H H H H

H Η Η Η 3 in compound 83, taking r3 and R4, and taking R10 and R11 together with -〇CF20- to form 2,2-difluoro [d] 1,3-benzodioxolane. In the compound material, the compound of formula I, wherein A is C, forms a hexahydropyridine ring; η is 0, forms a double bond between the methyl carbon (a) and the 4-position of the hexahydropyridine ring; m and ρ system 0; q system 0 and r system 1, forming N-oxides; and s system 1; E system-(CR27R28) x- (CR29R3〇) y- (where X system 1 and y system 0); R8 system Phenyl substituted with R22, R23, R24, R25 and R26; B is phenyl substituted with R9, R10, Rn, R12 and R13; of which R2, R5, R6, R9, R12, r13, R25, R26, R27 &amp; R28 series hydrogen; R24

R11 -97- 90038 200427680 Compound No. R3 R4 R22 R23 R24 R10 R11 86 Η cf3 HH Br Η cf3 87 Η cf3 FH Br Η cf3 88 Η Cl FF Η Η 89 Η FFF Η Η 90 Η cf3 FF Η Η 91 Η Cl H 〇ch3 Η Η 92 Η FH 〇ch3 Η Η 93 Η cf3 H 〇ch3 Η 94 Η cf3 H oc2h5 5 cf3 95 Η cf3 H oc3h7 Η cf3 96 Η 〇cf3 H 〇c3h7 Η OCF; 97b * -OCF2CF * -OCF2CF2- 98 Η cf3 HH cyclopropylmethoxyΗ cf3 99 Η cf3 HH c〇2c2h5 Η cf3 100 Η cf3 HH C02CH (CH3) 2 Η cf3 101 Η cf3 HH nhco2c2h5 Η cf3 102 Η cf3HH NHC02 103 Η cf3 HH NHC02CH (CH3) 2 Η cf3 104 Η cf3 HH nhco2ch2ch (ch3) 2 Η cf3 105 Η cf3 HH 1,3-thiazol-2-ylmethoxyΗ cf3 106 Η cf3 HH pyridine-2-oxy Η cf3 107 Η cf3 HH 5-muryl ^ 7 Biyodo-2-oxyΗ cf3 108 Η cf3 HH 6-chloropyridine-2-oxyΗ cf3 109 Η cf3 HH 3-trifluoromethylpyridine-2 -Oxy hydrazone cf3 110 Η cf3 HH 5-trifluoromethylpyridine-2-oxy hydrazone cf3 111 Η cf3 HH 5-night hydroxypyridine-2-oxy hydrazone cf3 112 Η cf3 HH 2-methyl -2fluorene-tetrazol-5-ylfluorene cf3 90038 -98- 200427680 Compound number R3 R4 r22 R23 R24 R10 R11 113 H Cl HH 2-ethyl-2H-tetra-5--5-ylfluorene Cl 114 H cf3 HH 2- Ethyl-2H-tetra. Zy-5-ylpyrene cf3 115c -〇cf2〇- HH 2-ethyl-2pyrene-tetrapyre-5-yl-OCF20-6 In compound 97, take R3 and R4, and take rh ^ rii and _〇CF2CF2_ I forms a 2,2,3,3-tetrafluoro-2,3--IL benzo [b] squeak ring, where the asterisk represents the point of continuation at R3 and at rig. ° In compound 115, take R3 and R4, and take RiO and Rii with _〇CF2〇- 一二 Fluoro "dll, 3-benzyl difluorene __ compound of formula I, where A is C, forming hexahydro Pyridine ring; η is 0, a double bond is formed between the methyl carbon U) and the 4-position of the hexahydropyridine ring; m and ρ are 0; r is 0 and q is 1 to form an N-disubstituted derivative ; And s series 1; e series-(CR27R28) x- (CR29R3〇) y- (where X is 1 and y is 0); R8 is phenyl substituted with R22, r23, r24, r25 and R26; B is A benzyl substituted by R9, R1g, R11, R12 and R13; of which R2, R3, R5, R0, R9, R10, R12, R13, R22, R25, R26, R27 and R28 are hydrogen; R24

90038 -99- 200427680 Compound No._ R4_ R7 R11 r24 -__ OCRFi_jKC3H7Q) PhCH2_OCHFg_OC3H7 Compound of formula I, where A is C, forming a hexahydropyridine ring; 0, at the 4-position of methyl carbon (a) and π-hydropyridine ring Double bonds are formed between them; m, 9 and 1 * are 0; s is 1; P is not 0 to form an azabicyclic derivative; r8 is a phenyl substituted with r22, r24, R25, and R26; HMCRnR28McR29R30v ( Wherein y is 〇); B is phenyl substituted with R9, Ri0, Rii, Ri2 and Rl3; where R2, R3, R5, R6, R9, R10, R12, Rl3, R22, r23, r25, r26 , R27 and R28 series hydrogen: R24

The compound of formula I 'wherein eight systems c form a hexahydropyridine ring; n series 0, a double bond is formed between the methyl carbon (a) and the kernel position of the hexahydropyridine ring; ㈤ system 0; q &amp; r system 1,幵 y into an N "'disubstituted oxy derivative; P is not 0, forming an azabicyclic derivative; · is a phenyl substituted with RU, r23, RM, and R26; it is represented by R, R, R, Rl2 And R13 substituted phenyl; and E series- (CR27R28) x- 90038 -100- 200427680 (CR29R3G) plant (where X series 1 and y series 0); among which R2, R3 ,, R6, R9, R10, R12, R13, R22, R23, R25, R26, R27 and R28 are hydrogen: R24

R11 Compound No. R4_r7_Dp R11_R24 1185 CF3 C2H4CO2C2H5 -CH2- 3 CF3 Pyridin-2-oxy compound of formula I, in which A is C and forms a hexahydro leaf I: lake ring; m, p, q and r are 0; s is 1 η is 0, a double bond is formed between the methyl carbon (a) and the 4-position of the hexahydropyridine ring; R8 is a pyridin-3-yl substituted with R22, R24, R25, and R26; E is-(CR27R28 ) x- (CR29R30) y- (where X is 1 and y is 0); B is R9, R10,

Rn, R12 and R13 substituted phenyl groups; of which R2, R3, R, R6, R9, Ri0, R12, R13, R22, R25, R26, R27 and R28 are hydrogen: R24

RU 90038 -101-200427680

Compound number R4 R11 R24 119 cf3 cf3 C1 120 cf3 cf3 〇c3h7 121 cf3 cf3 ON 122 cf3 cf3 nhc3h7 123 cf3 cf3 nhco2c2h5 Compound of formula I, wherein A is C, forming a hexahydropyridine ring; m, p and q are 0; s System 1; η system 0, which forms a double bond between the methyl carbon (a) and the 4-position of the hexahydropyridine ring; r system 1, which forms an N-oxide; R8 is substituted with R22, R24, R25, and R26 Said Yodo-3-radical; E-series-(CR27R 28) x- (CR29R3G) y- (where X-series 1 and y-series 0); B-series is replaced with R '9, Ri0, Rn,] R12 and R13 Phenyl; wherein R2, R3, R5, R6, 'R9, R10, R12, R13, R22, R25, R26, R27 and R2S are hydrogen; R24

R11 90038-102-200427680 Compound number R4 R11 r24 124 cf3 cf3 Cl 125 cf3 cf3 〇c3h7 126 cf3 cf3 C = N 127 cf3 cf3 nhc3h7 128 cf3 __cf3 nhco2c2h5 The compound of formula I 'wherein A is C- 幵 y 1 Dihydro p ratio ring; m, p, q, and r are 0; s is 1; η is 0; a double bond is formed between the methyl carbon (a) and the 4 · position of the pyridine ring; E- (CR27R28 ) X- (CR29R30) plant (where X is 1 and y is 0); is a phenyl substituted with R22, R23, R24, R25 and R26; B is a phenyl substituted with R9, Rio, Rn, Rl2 and Rl3 ; Of which R2, R3, R5, R6, R9, R10, R12, R22, R23, R25, R26, R27 &amp; R28 are hydrogen;

R11 90038 -103- 200427680 Compound No. R4 Rn R24 129 cf3 Br 〇C3H7 130 cf3 F NHC02C2H5 131 cf3 cf3 c〇2c2h5 132 cf3 cf3 Ye Dian Dian-2-Mulyl 133 Cl Cl 2-ethyl-2H-tetrazole- 5-yl 134 cf3 Cl 2-ethyl-2H-tetrazol-5-yl 135 cf3 cf3 2-ethyl-2H-tetrazol-5-yl 136 cf3 〇cf3 2-ethyl-2H-tetrazole- 5-based compound of formula I, in which A is C and forms a hexahydro p ratio ring; p, q, and r are 0; m and s are 1; η is 0, at the methyl carbon (a) and the hexahydropyridine ring A double bond is formed between the 4-positions of E; E- (CR27R28) X- (CR29R3G) plant (where X is 1 and y is 0); B is the bridging group from methyl carbon to R; R8 is based on R22, R23, R24, R25, and R26 substituted phenyl; R is a phenyl substituted with R17, R18, R19, R2G, and R21; of which R2, R3, R5, R6, R1 ?, R18, R2O, R21, R22, R23, R25, R26, R27 and R28 are hydrogen; R24

90038 -104-

I 200427680 Compound number R4 B R15 R19 r24 137 〇cf3 〇-- 〇cf3 2-ethyl-2H-tetrapent-5-yl 138 cf3 ch2 — cf3 OC3H7 139 cf3 ch2o — cf3 nhco2c2h5 140 cf3 〇ch2 — cf3 ch = noc2h5 141 cf3 〇ch2ch2o-cf3 OC3H7 142 Cl OC (= 〇) NR15 H Cl pyridine-2-oxy143 cf3 〇C (= 0) NR15 H Cl pyridine-2-oxy144 〇cf3 0C (= 0) NR15 H cf3 pyridin-2-oxy145 cf3 0C (= 0) NR15 H cf3 2-ethyl-2H-tetrazol-5-yl 146 cf3 nr15s〇2 H cf3 compound of formula I, wherein A is C to form a 1,4-dihydropyridine ring; p, q, and r are 0; m and s are 1; η is 0; a double bond is formed between the methyl carbon (a) and the 4-position of the pyridine ring; E series- (CR27R28) x- (CR29R30) y_ (wherein the fluorene series i and y series 〇); b is the bridging group from methyl carbon to R; R8 is benzene substituted with R22, R23, R24, R25 and R26 R is phenyl substituted with R17, R18, R19, R20, and R21; of which R2, R3, R5, R6, R17, R18, R20, R21, R22, R23, R25, R26, R27

R 丨 9 90038 -105- 200427680 Compound No. R4 B R15 R19 R24 147 cf3 〇— cf3 p ratio -2-oxyl 148 cf3 ch2 — cf3 〇c3h7 149 cf3 ch2 — cf3 c〇2c2h5 150 Cl ch2 — Cl nhco2c2h5 151 〇cf3 ch2 — cf3 NHC02C2H5 152 〇cf3 ch2 — 〇cf3 nhco2c2h5 153 cf3 ch2o-cf3 nhco2c2h5 154 cf3 0C (= 0) NR15 H cf3 2-ethyl-2H-tetrazole-5-yl compound of formula I, of which A System CH, forming a hexahydropyridine ring; η system 1, forming a single bond from methyl end (a) and its substituents; p, q and r are 0; m and s are 1; B is from methyl carbon to R Bridge base; E series- (CR27R28) x- (CR29R3G) y- (where X series 1

And y is 0); R8 is a phenyl substituted with R22, R23, R24, R25, and R26; and R is a phenyl substituted with R17, R18, R19, R20, and R21; wherein R1, R2, R3, R5, R6, R22, R23, R25, R26, R27 and R28 are hydrogen;

R4 R5 90038 -106- 200427680 166 CF3 OCK7 165nF, OHHNOC7H, 163 CF3 Wu Yan-2- 烨 ^ 164 CF \ 2 丨 0; &amp; 丨 2Hi ^ 丨 5 "162 nF3 2-p ^ i2H-s ϋ 161 OF3 2 丨 £ 丨 160nF3n02c2H5 159 CF3 Wu ^ 158 CF, OH &quot; NOC7H, 157 OF3 156 CF3 CO02 155 OCF3 OC3H7

κ Ηκffi K K I Shann K H K Ks HE FI HE

Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl

H Eaffi H ffi ffi ffi K E Kn Ht H HE Hf E K ^ r ^ 2; kso2 OC2H40 0Φ0

MRC ^ P o O O O Os S〇2 ffi

R 24 R`` / R A-

R 19

Rg / R-A

B 11-¾ 90038 -107- 200427680

178 OCF3 NHC02CH2iCH 177 OF3 NHC02CH2CH &quot; ciI2 176 OCF3 NHC02CH (CH3) 2 175 0F3 NHC02C2H5 17 厶 0nF3 n020ffi (nffi3) 2 173 OF3 002C2H5 172 CF3 OC2H0CH3 R 171HCF3 OCF3 OCH3 CF

K ffi E H H K K ffi H K E K H K K

Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl

H K En 1 Hill nnnffi Pi HEn K H K E K

oclro) NR 15 o c on (卩 0) 1NR ^ oo (ho) ^ r ^ on ^ nowi oclro) NR on ^ nowi ocllo) NR on? w§ oo (HO) 2n a 0! 00.0 24

H-7R 17 / dloo 19

Co 15 15 15 OH3 OH3 OH3 OH3 OH3 CH3 OH3 OH3 S3 ^ 5 / ^ 6 90038 -108- 200427680

191 OF3 OHnNOpHS 190 OF3 OH = NOC2H5

189 OF3 OH &quot; NOC2HS 188 CF3 CHHNOC2H5 18-JCF3 OHHNOC2H5 186 OF3 OKnsoffi 185 CF3 CH &quot; NOC2H5 184 OF, OHHNOOl · 183 OF, ΟΗΠΝΟΡΗ, 182 OF3 OH &quot; NOC2H5

180 CF3 0C (= 0) NHCH (CH3) 2 181 OCF3 4 ^^^ _ ά · Chicken llA 179 CF3 NH82C2H40CH3 K H H E H n n F H F E Cl Cl Et Cl Cl H Cl

Cl Cl F Cl Br H n FFH Cl Cl HHE ffi ihlh KKHHHKKH HE H ffi KKH ffi KK Cl oo (ho) mh oc (ho) nr 00 (= 0) 2:11 oclro) NR oclro) NR on? W§ 00 (卩 0) 21100 (卩 oclro) NR 〇0 (卩 〇) 11 15 15 15 15 15 0¾0¾ n ffi nn E ffi

R 24

R-VRS R a 5P21

Point B 15¾ 90038 -109- 200427680 2CM OF3 OHHNOC2H, 203 OF3 CHHNOC2H5 202 OF, chhnoph. 201 CF3 CHHNOC2H5 200 OF, ohhnoph. 199 OF3 IOC2H5 198 CF3 CHHNOC2H5 197 OF3nHHNOCH (CH3) 2 195 OOF3 OHH2002H5 194 ^ OOF, chhmooh. 193nF \ OH 卩 NOPH, 192 CF3 OHHNOC2H5

Cl K F ffi E F K F F ffi F F H F K H F F F F CF3 H H

Cl FFFFFHHKFFK Cl ffi ffis KEKFFFK 1 mountain FFKI mountain oclro) NR on? W§ ocno) NR on ^ HOW§ 00 (卩 0) -11 on (HO) NR ocno) NR on (HO) ^ Il ocho) nr on? w§oo (HO) Mn 15 15 15 15

nffi E ffi PC ffi ffi ffi K

R 24 R`` / R 叾

R 19

Rg / Re

B R-VR-. 90038 -110- 200427680 217 OF3 6 丨 0 | Miscellaneous-2 丨; &amp; 216 CF3 disease-2-off 215 CF3 4 丨 Cl 丨 wu disease 丨 2 丨 ^ 2M CF3 OH &quot; NOC2H, 213 C, F3 〇ΪZO 212 OF3 OH = NOp® 211 CF3 OHHNOC2H5 210 OF3nH &quot; NOC2H, 209 OF3 OHHNOC2H5 208 CF3 CHHNOC2H5 207 CF3 CHHNOC2H5 206nF3 OHHNOC2H5 205 CFy CHHNOC2HCF 3H 0F 0F 0F 0F H &amp; ffi QHH Cl ffi 01

E Et 1 Hills K K H ffi K Cl Kn Ea ϋ K K K ffisffi K

0CIT02R ocno) NR oc (no) NR 00¾¾ ocirozR oc (ho) nr 00 (卩 0) ^ R on (卩 o) MR on? WiociroNR ocllo) NR oclro) NR

JH HE E K K K ffin E

R 24 173 100 R one

Rg / Re

B R-VR = 90038 -Ill-200427680 230 CF33b Bureau 12-¾ ^ 2280F3 ^-^ 12-^^ 229 CF3 ^ -Illness 2--2- ^ 226 OCFa Wu ^ · 2-ιι; &amp; 225 OPh Wu Yan -2-ILi 224- SF5S · ^ 丨 2 丨 ^ '^ 223 ΝΌ2 ^^ ι2 * ^^ 222 F 矣 焱 -2- ^ ¾ 221 181 ^^ 121¾ ^ 220 CF3 2- (c3H70 ¥ s-; &amp; 219 CF3 5 丨 CF3 ^ b disease-2 丨 w &gt; 218 CF3 5-CH30 ^: b way-2 ~ Office ffiκ Hn H Etnnm Hnffi HK HE H Cl Cl Cl Cln

Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl Cl Cln Cl Cl KK ffi K Htnnffi IInn K ffi ffi ffinffin HK ffi K ffi ffi oclro) NR oo? W§ OO ^ HOW§ 00? W§ ^ ocno) NR = 0C1I0) NRC; on (卩 o) zn ociro) NR on ^ HOW2 ^ oclro) NR. oc (ho) nrg; oclro) NR. oc (&quot; o) NR-) 15 15 15 15 ffi 0¾ 0¾ 0¾ H K ffi 24 19

Rg / Re

B R-VR One. 90038 -112- 200427680 243 CF3 奂 硌 -2-il ^ 242 OF3 Wu Wei 丨 2 丨 ^^ 241 OF3 Wu ^ -2- | 14 240 cf3s- ^ i2 ~ ^ \ j ^ 239 CF3 238 0CF3 Wu Yan-2 -| 1 ^ 237 OF3 Wu 硌 丨 2- | 1 ^ 236 OCF3 Wu 硌 —2 · ^^ 235 OCF3 Wu ^ -2 · ^^ 2M CF3 奂 为 -2 丨 233 CF3 Wuyi-2- 烨 唞 232 C5 231 OF3奂 is -2- | 1 ^

Cl Cl ffin Cl Cl Ht Cl F ffi K H F K F F F IF E F F F

H E K Cl K F F F K F F

ffi Cl H Cl ffi ffi Cl Cl ffi ffi KH ffi F ffi Faffi F ffi ffi F on (卩 0) 211 ocno) NR ocnCONR ocnCONR 000-0) 2:11 oo ^ nnow ^ on? w§ 000-0) ¾ ^ on? w§ ocnCONR OOTOW§ oclro) NR on? w§ ffi ffi ffi ffi KK ffi ffi ffi ffi ffi ffi ^ §§Μβ ^ 24 19

Rg / RN-1

B R-VR-. 90038 -113- 200427680 256 Q3 One 丨 -¾¾W f 3 丨 _ 255 OF Two_s 丨; One: 252 CF3 桊 £ 丨; One: 253 CF3 丨; £ 250 CF33b Road—2-¾ ^ 246 OCF3 Wu ^ v-2_il ^ 247 0F3 Wu £-| 1 ^ 248 CFW Wu ^ 249 CF3 Wu Wei 丨 2- | 一; &amp; 245 OF Second E 丨 2 · # ι ^ 2έ QF3 奂 硌 丨 2 丨! l ^

F K CF3 Η ffi Η ffi CF3 ffi CF3 ffi ffi H H K H ffi H E 1 mountain ffi E E H

H nF3 CF3 Q ffi §3 舛 A Cl Q 01 Q Q

F ffi HHK s CF3 H ffi KKKHKHKKK ffi KH on ^ HOW§ 0η (Η0) ζΙι 00 (卩 0) 的 onon (卩 C02H on ^ HOWZ ^ 00¾¾ on (HO) ^ n oochgo ^ r 00 (卩 0) 2 : 穴 occhcomuocllo) NR OO ^ HOWi OO ^ HOWi H ffi FI KK ffi ffi EK ffi ffi

R 24

R3 / R 100

Rg / Re

B R-VR One. 90038 -114-200427680 269 OF3 2 丨 &amp; 丨 2υι4ϋ 267 OCF3 2-6; &amp;: 2H-s ^ -5 丨; 1: 266 OCF3 2--9; &amp; -2Η-3 ^ ϋ 264 Cl 2丨 f Office 丨 2Hi ^ 丨 5 丨 Office 263 0C, F3 2— f ^ -2H-sbl--5- ^ 261 OCF3 2-c ^^-2h-q ^ -5- ^ 257 CF3 5-f 258 OF3 4 丨 f | l; one: 丨 li-x 备 备 -3A 259 CF3 8— f #l?, 2,3,4-sas-5 丨 260 OF3 ffi ffi ffi ffi ffi ffi ffi H ffi ffi Cl ffi H Cl ffi E Hn KK Br ffi

Cl Cl Cl Clnffiffi Q Cl Cl Cl E Br

I Hill EHKK ffi HEK ffi K PI KKKHHK on? Wi ocno) NR ocno) NR ocno) NR oc (&quot; o) NR oo (HO) 2Fl oclro) NR oc (no) NRocllo) NR on ^ HOW§ oc (ho ) nr oc (HO) ^ n oc (ho) nr ffi KE ffin K ffi E ffi ffi

R 24

P7R 17 / dloo R one

Rg / R- 一 ro ^ 1¾ 90038 -115-200427680

282 C, F3 2-c ^^-2H-Qbl--5-; iL 280 CF3 2-21 &lt; ^-2H-lEy Fen-5-¾ 281 CF3 2 * ^ Support-5-¾ 279 CF3 278 OCF3 2 -f ^, 2H-s ^ l5 丨; one: 277 OCF3 2 丨 6 ^ · 2η-3 ^ -5- ^ 276 &quot; OCF3 2 丨 f _-2h-3 ^ 丨 5 · &amp; 275 OCF3 2- f ^ -2H-s ^ -5 丨; &amp; 274 Cl 2—ί—2Η-? Κ-; &amp; 273 OCF, 2-f; sl-2h-q ^ -5-1: 272 OCF3 2if ι: · 2η-3 ^ -5- ^ 271 OCF3 2 丨 61L.2H 丨 a ^ -5 丨 4 270 OCF- 2-(&gt; ^-2H-shl--5 · ^ ffi KKHKFH ffi FKHHHHH Cl Cl Cl ffi Cl Cl HFFFFF ffi Cl ffi

Br ffi ffi K ffi H JH H H H Hm H H ffi ffi K K ffi Cl En

on (卩 o) NH ocno) NR ooc-CONn 00 ^ 0¾ oolro) NR οη (ΗΟ) ΝΙι 00 ^ 0¾ ^ 00¾¾ ocxhconh 00¾¾ οηο = ο) ΝΙι 00¾¾ ocllo) NR ffi ffi K ffi ffi ffi ffi ffi ffi ffi -24 R3 / R a-

Hole B 5¾ 90038 -116- 200427680 294- OCF3 2--¾ ^ 丨 2H—S ^ 丨 5 丨 Office 295 OCF3 2-6; &amp; -2H-s ^ -5 丨 驷 293 QF3 2-6i-2Hi -5--5- 292 OF3 2 丨 6 ^ -2Η—3ι4-hand 291 OCF3 2 &gt; c ^^-2H-sl4-5 丨 i 290 OCF3 2—f ^ -2H-s ^, 5-i 285 OCF3 2 -6i-2H—0 ^ -5-i 286 OCF3 2-c ^^-2H-s ^ -5- ^ 287 OCF3 2-p ^. 2H-s ^ l5— ^ 288 CF3 289 CF3 2- 6 Drop- 5-¾ 284 CFJ2 丨 2LJ ^ —2H-® ^ 丨 5— ^ 283 CF3 2-o Η ffi Q m 01 I mountain Hmffi K HCF3 HHKHH ΙμΗ0F3 H 0F3 ffin Q H0H3nn (CH3) 2S3n0F3CF3 0F3 Q0CF3 OOF,

Cl ffi ffi Cl H Haffi K Hn X ffin K K K CF3 H Kn

οηΎΟ ^ oclro) NR 0CIT02R 00¾¾ ocno) NR oc (ho) nr ocno) NR 00¾¾ 000 = 0) 211 οηΎΟ ^ on? w§ onllo) NR oclro) NR n K IHiH K K E ffi ffi ffi ffi

R 24 R a ^ 0¾

Point B 15¾ 90038 -117- 200427680 308 OOF3 2-p ^ -2H, @ hl--5 丨 _ 307 OCF3 2-d.-2H-al4-5 丨 i 306 OCF3 2 · τ ^ -2Η-β ^- 5 丨; &amp; 305 OCF3 2-6¾ 丨 2H-0 ^ -5 丨; 1: 304 OCF3 2-p ^ -2H-s ^ -5 丨; ^ 303 OF3 C002H5 302 OOF3 2-(^ 1: -2Η -0 ^ -5— ^ 300 OF3 2 丨 f; &amp; —2Ηέ 丨 5—i 301 C'F3 2 丨 碉 一: -2H-shl--5-; &amp; 299 OF3 2 丨 d: 丨 21 Mountain 丨 No. 1 丨 5 丨; &amp; 298 CF3 2-D -5--5- 297 c ^ 2-61L-2H-3 4i-5-; &amp; 296 OCF3 2-6_-2H-Q ^ -5 丨; &Amp; ffi E ffi K ffi H ffi HHHHHK ffi H ffi ffi H ffi

No- do!蝌 αα Q nF3 Q OF3 OQ3 2 丨 诮; &amp; -2H—3 different 丨 5 丨 _ CF3 OCF3 I mountain sn HH ffi En KHHHKK ffi KK a ffi K ffin oc (&quot; o) NR a ocno) NR a oclro) NR. ocno) NR-nH2 nH2cn0) 2: Rc; 0CH2C (H0) NR = ocns) NR-0H2 00¾ 00¾ 00¾ OOHO) OO (HO) -15 15 K E K ffi

R 24 R`` / R 1⑺ η 19

B R one VR one. 90038 -118- 200427680 321 OCF3 2-^^ · 2Η-0 ^ έ 320 OOF3 2-f ί: -2Η-3 ^ ϋ 319 OOF3 2--91: -2h, 3 ^ -5- ^ 317 OCF3 2— f i-2H-Q ^ -5 · ^

316 OCF3 2l ^^-2H-Qbl--5-; SL 3150CF3 2 丨 f ^ -2H-s ^ -5-; &amp; 3M OCFd2 丨 f _—2H 丨 s ^ 丨 5 丨; &amp; 313 OCF \ 2--6 ^ -2H-@ ^ l5 · ^ 312 OCF- 2-f ^ -2H-s ^ .5l ^ 310 OCF- 2 ,; &amp; -2h-0 ^ -5- ^ 311 OCF3 2-f 4l2H-s ^ -5- ^ 309 OCF- 24_-2Ηέ ^ -5 丨 _

Cl u ffi Cl n ffi F K F ffi K ffi H H nH3 00¾ OOF3No-

K ffi Cl Br ffi ffi F n K H n E E ffi K K E ϋ H K H I Mountain H K H n NR ^ CIIO) 2R-0H2 NR-rrH2 NR-nH2 MR3; nffi2 NR-0H2

K ffi ffi ffi HE K ffi ffi K 24

R 19

Rg / RW-1

BR one set 16 90038 -119- 200427680 3M OCF3 2 丨 f; &amp; 丨 2H 丨 丨 5-1: 333 OCF3 2-τ ^ · 2η-3 ^ -5- ^ 332 OCF3 2—f i-2H-a ^ -5- ^ 331 oc ^ 2-^^-2H-s ^ -5 * ^ 330 OCF3 24 ^ -2Η · 3ι4 丨 5 丨 _ 329 0CF3 2 丨 fi—2H 丨? jk 丨 5 丨 i 328 OCF \ 2-f ^ -2H-Q ^, 5— ^ 327 OCF \ 2—f 1l-2h-s14-.5- ^ 326 OCF, 2_f ^ | 21 山 | 0fen | 5丨 ^ 325 OCF3 2-fi 丨 2Η, β ^ ι5- &amp; 32 仁 OC712 丨 f; &amp; 丨 2? @ 朵 丨 5 丨 _ 323 〇CF, 2-f ^ -2H-0 ^ -5— ^ 322 OCF \ 2-^^-2H ~ 3 ^ -5- ^

Cl Cln H K F ffi H F H H ffi H H E H H H ffi H Cl

OH3 onffi3 0nF3 202 K

s Cl Br K F

n K Hs ϋasffi H K K H ffi H H ffim H K ϋ H

NR-n (HO) NR

2:11 MR _ MR MR MR NR MR. 2R PHO) nno) nHo) eHo) ecno) OHO) PHO) O ^ (HO) nHo) OHO) n (HO) elro) 24

R 19

Rg / R-A

B 16

nffiffin KX ffi KR-VR5 90038 -120- 200427680 347 OCF3 2ϋ-2Η-3 ^ -5 丨 _ 344 OCF3 2-f; SLMHISbl-l5- ^ 345 0C, F3 2-f ^ -2H &gt; s ^ -l5 丨; 1: 346 OCF3 2--3 ^ -2H-s ^ -5 丨 Office 343 OCF, 2 · ^^-2η-3 ^ · 5-; 1: 340 OCF3 2-f ^. 2H-shl--5 -; iL 341 OCF3 2 * f i-2H-sbl--5- ^ 342 OCF3 2--6 ^ -2H-s ^ ~ 5- ^ 339 〇CF, 2-f ^ -2H-sbl--5_ ^ 338 OOF, 2 * f _-2Η-0 ^ ϋ 337 0C3 2 * f ^ -2HIS ^ 丨 5 丨: &amp; 335on ^ 2--Q ^ -2H, s ^ -5- ^ 336 CF, 2- f ^ -2H-0 ^ .5l; &amp; Η Cln K ffi F ffi HF Hmn Hnn HHHK HE Cl

ffi Q Br H ffi F I S3 OOH3 S3 OOF3 202 K K ffi I mountain H H ffi ffi H H H H ffi K H K ffi Et ffi ffi K H ffi NR -nlro) NRg NR -nHoo NR-nlro) NR 叾

NR = cno) NRS NR -n (HO) NR 叾 NR -c ^ lro) NR -NR -c ^ llo) NR -NR ^ Cno) NR -NR 2 clro) NR -NR -rrno) NR -NR-- cno) NR -NR -nlro) NR -NR ^ CITo) NR -90038 ιιο 200427680 357 OCF3 2- f; sl. 2h-s ^ -5-; sl 358 OCF3 2--9l: l2H-sbl-- 5- ^ 356 0C, F3 2 * f ^ -2Η-0 ^ · 5 丨; &amp; 3M OCF3 2 丨 f; &amp; 丨 2H-a ^ —5 丨; 1: 355 OCF3 2 · f i-2H- s ^ -5 丨; &amp;

353 OCF3 2— f! L-2H-Q ^ -5-; iL 351 OCF3 2-^^-2H 丨 3 ^ -5-¾ 352 OCF3 2lfi: 2H-s ^ -5 丨 &amp; 350 OCF- 2 · F ί: -2Η · 0 ^ -5— ^ 349 OCF3 2-^^-2h-s ^ i5- ^ 348 OCF3 2-f ^ -2H-S ^. 5-1:

H Cl K ffi F E F H H ffi K K K K K H E K OH3 OS3 OCF3 202

ffi Cl Br FKKK ffin H PIs H Kt KH FI KK IHiH ffi Et NR-n (6) 0 NR-nlloo NR ^ Cnoo NR-niloo nr ^ choo NR ^ Ciroo NR ^ CIIOO NR ^ Cnoo NR-nHoo NF ^ Clroo NR -n (HO) o I nffi KKK ffi 24

Rg / Rt

B ^ 16 16 90038 -122- 200427680 The fine compound 'wherein A series CH' forms a hexahydroton ring; read ", forming a single bond from methyl hard (a) and its substituents; p, q &amp; r series. m &amp; s is 1; b is the bridging group from methyl carbon to R, where B is OC (= 〇) NR15; E is-(CR27R28) x- (CR29R3〇) y- (where X is 1 and y is 0); R8 is a phenyl substituted with R22 'r23, r24, r25, and R26; and &amp; is a phenyl substituted with 1117, r18, R19, R2G, and r21; wherein R2, R3, R5, R6, R15, R17, R18, R20, R21, R, R23, R25, R26, R27 and R28 are hydrogen:

R4 R5 Compound number R1 R4 R19 R24 359 ch3 cf3 H CH-NOC2H5 360 ch3 cf3 Cl CH = NOC2H5 361 ch3 ocf3 Cl ch = noc2h5 362 CH (CH3) 2 cf3 H ch = noc2h5 363 ch (ch3) 2 cf3 Cl noc2h5 364 ch (ch3) 2 〇cf3 Cl ch = noc2h5 365 ch2〇ch3 cf3 H ch = noc2h5 366 ch2och, cf3 Cl ch = noc2h. 90038 -123- 200427680 Compound No. R1 R4 R19 R24 367 CH2OCH3 OCF3 ClF3 Cl Phenyl cf3 H ch = noc2h5 369 Phenyl cf3 Cl ch = noc2h5 370 Phenyl ocf3 Cl ch = n〇c2h5 371 ch3 cf3 H Leaf Dike-2-oxy 372 ch3 cf3 Cl Outer Dike-2-oxy373 ch3 ocf3 Cl Ye Dian-2-oxy374 CH (CH3) 2 cf3 H p ratio lake 2-oxy375 CH (CH3) 2 cf3 Cl p ratio lake 2-oxy376 CH (CH3) 2 ocf3 Cl Leaf Dike-2-oxy 377 ch2och3 cf3 H Outer Dike 2-oxyl 378 CH20CH3 cf3 Cl Leaf Dike 2-oxyl 379 CH20CH3 ocf3 Cl p than Bitoxy-2-oxy 380 phenyl cf3 H Ye Zhidian-2-oxy381 phenyl cf3 Cl outer Zhidian-2-oxy382 phenyl ocf3 Cl pyridine-2-oxy383 ch3 cf3 H 2-ethyl-2H-tetrat-5-yl 384 ch3 cf3 Cl 2-ethyl-2H-tetrazol-5-yl 7385 ch3 ocf3 Cl 2-ethyl-2H- Tetrazol-5-yl 386 CH (CH3) 2 cf3 H 2-ethyl-211-tetra-5-yl 387 CH (CH3) 2 cf3 Cl 2-ethyl-2H-tetrazol-5-yl 388 CH (CH3) 2 ocf3 Cl 2-ethyl-2H-tetrazol-5-yl 389 ch2och3 cf3 H 2-ethyl-2H-tetrazol-5-yl 390 ch2och3 cf3 Cl 2-ethyl-2H-tetra17 -5-yl 391 CH20CH3 ocf3 Cl 2-ethyl-2H-tetrazol-5-yl392 phenyl cf3 H 2-ethyl-2H-tetrazol-5-yl 393 phenyl cf3 Cl 2-ethyl-2H -Tetrazol-5-yl394 phenyl ocf3 Cl 2-ethyl-2H-tetrazol-5-yl compound of formula I, in which eight are CH to form a hexahydropyridine ring; η are 1, from methyl carbon (a ) And its substituents form a single bond; ρ is 0; q is 0 and Γ is 1 to form N-oxygen 90038 -124- 200427680 compounds; m, s and r are 1; B is a bridge from methyl carbon to R Base, where b is 〇C (= 0) NR15; E is- (CR27R28) X- (CR29R30) plant (which is also 1 and 7 is 0); R8 is replaced by R22, R23, R24, R25 and R26 Phenyl; and R is phenyl substituted with R17, R18, R19, R20, and R21; of which R1, R2, r3, r5, R6, R15, R21, R22, R23, R25, R26, R27, and R28 are hydrogen:

R4 R5 Compound number R4 R17 R18 R19 R20 R24 395 cf3 HH Cl H pyridin-2-oxy396 cf3 H Cl Cl H pyridin-2-oxy397 cf3 HFHF pyridin-2-oxy398 cf3 HH cf3 H pyridin-2 -Oxy 399 ocf3 HH Cl H 2-methyl-2H-tetrazol-5-yl 400 〇cf3 HHFH 2-methyl-2H-tetrazol-5-yl 401 cff3 HHFH 2-ethyl-2H-tetra Spit-5-yl 402 ocf3 HH cf3 H 2-methyl-2H-tetrazol-5-yl 403 ocf3 HH cf3 H 2-ethyl-2H-tetrazol-5-yl 404 cff3 HH ocf3 H 2-methyl -2H-tetrazol-5-yl 405 cff3 HH 〇cf3 H 2-ethyl-2H-tetrat-5-yl compound of formula I, in which A is CH and forms a hexahydro leaf 1: fluorene ring; η system 1, forming a single bond from methyl 90038 -125- 200427680 carbon (a) and its substituents; p, q &amp; r system 0; m &amp; s system 1; B system is a bridging group from methyl carbon to R, where B 〇; E series- (CR27R28) x- (CR29R3i)) y- (where X is 1 and y is 0); R8 is phenyl substituted with R22, R23, R24, R25 and R26; and R is R18 , R19, R20, and R21 substituted pyridin-2-yl; wherein R2, R3, R5, R6, Ri7, Ris, R2i, R22, r23, r25, r26, r2? And R28 are hydrogen:

Compound number R1 R4 R19 R20 R24 406 Η cf3 ocf3 H OCH (CH3) 2 407 Η cf3 cf3 H NHC02CH (CH3) 2 408 Η cf3 cf3 H 2-methyl-2H-tetrazol-5-yl 409 Η cf3 cf3 H 2-ethyl-2H-tetra-sigma-5-yl 410 ch3 ocf3 cf3 H 〇C3H7 411 ch3 cf3 cf3 H ch = noc2h5 412 ch3 cf3 HF 2-ethyl-2H-tetrasial-5-yl 413 CH (CH3 ) 2 cf3 Cl H c〇2c2h5 414 ch2〇ch3 cf3 FH leaf dagger-2-oxy415 phenylmethyl cf3 Br H 〇c3h7 90038 -126- 200427680 A compound of formula I, wherein A is C and forms 1, 2 , 5,6-Tetrahydropyridine ring; η system 1, forming a single bond from methyl carbon (a) and its substituents; p, q &amp; r system 0; 111 and 3 system i; B system from methyl carbon to Bridging group of R; e- (CR27R28) x- (CR29R30) y- (where X is 1 and y is 0); R8 is phenyl substituted with R22, R23, R24, R25 and R26; and R is based on R17, R18, R19, R20 and R21 substituted phenyl groups; wherein R1, R2, R3, R5, R6, R22, R23, R25, R26, R and R28 are hydrogen:

I Bulletin 5 Tiger R4 R19 B R15 R24 416 cf3 cf3 0 —Pyridine-2-oxy 417 cf3 cf3 s — CO2C2H5 418 cf3 cf3 ch2 —10C3H7 419 cf3 cf3 ch2〇nhco2c2h5 420 cf3 cf2 och2 — ch = noc2h5 421 cf3 cf3 〇ch2ch2〇- 一 〇c3h7 422 Cl Cl 0C (= 0) NR15 Η pyridine-2-oxy 423 cf3 Cl 0C (= 0) NR15 Η p ratio lake 2-oxy 424 ocf3 cf3 0C (= 0) NR15 Η p Biyodo-2-oxy 425 cf3 cf3 0C (= 0) NR15 Η 2-ethyl-2H-tetraki-5-yl 426 cf3 cf3 NRl5S02 Η 比 Biyodo-2-oxy Group 90038 -127- 200427680 A compound of formula I wherein A is CH and forms a hexahydro p ratio ring; with system 1, a single bond is formed from methyl carbon (a) and its substituent; p, q and r are 0; System 1; b is the bridging group from methyl carbon to R; E is-(CR27R28) x- (CR29R3〇) y_ (where continued) and y is 0); and R8 is R22, R23, R24,: ^ And ^ substituted phenyl; wherein R2'R3, R5, R6, R22, R23, R25, r26, r2ir28 are hydrogen:

Compound number R R4 B R15 R24 427 c3h7 CF3 -0C (= 0) NR15. H Pyridine-2-oxy 428 CH (CH3) 2 Cl -0C (= 0) NR15- H 17 CH (CH3) 2 CF3 -0C (= 0) NR15- H Pyridine-2-oxy 430 CH (CH3) 2 〇cf3 -oc (= o) nr15_ H koubidian-2-milk 431 ch2ch = ch2 CF3 -0C (= 0) NR15- H Pyridine-2-oxy432 Cyclohexyl CF3 -0C (= 0) NR15- H Mouth Biyodo-2 * • milk 433 c3H7 〇cf3 -NR15S〇2- H 2-form -2H-tetrazol-5-yl compound of formula I, in which eight systems of CH form a hexahydro p ratio ring; η system 1, forms a single bond from methyl carbon (a) and its substituents; p, q and r is 0; m and s are 1; B is a bridging group from methyl carbon to R; wherein R is pyridin-2-yl substituted with R18, R19, R20, and R21; E is-(CR27R28) x- ( CR29R30) y- (where X is 1 and y are 0); and R8 is a benzyl group substituted with R22, R23, R24, R25, and R26; Ri, R2, 90038 -128- 200427680

Compounds: Wanhu B R4 R19 R20 R24 434 〇ocf3 cf3 H 2-methyl-2H_tetrasal-5-yl 435 〇cf3 Cl H 2-methyl-2H-tetra-5-yl 436 〇C (= 0 ) NR15 * cf3 HH pyridine-2-oxy 437 〇cf3 cf3 H pyridine-2-oxy 438 0 cf3 H cf3 pyridine-2-oxy 439 〇C (= 0) NR15 * cf3 Cl H pyridine-2-oxy 440 0 cf3 cf3 H 6-aminopyridine-3-oxy 441 〇cf3 H cf3 6-aminopyridine-3-oxy * R15 is a hydrogen compound of the formula I 'wherein the A group CH' forms hexahydrop Bidian ring; n system 1, forming a single bond from methyl carbon (a) and its substituents; ρ system 0; m and s system 1; q system 0 and I * system 1, forming N-oxide; B system Bridging group from methyl carbon to R; where r is an orbital-2-yl group substituted with R18, R19, R20, and R21; E is-(CR27R28) x- (CR29R3〇) y * (where X is 1 And y is 0); and R8 is phenyl substituted with R22, r23, r24, R25, and R26; of which R1, R2, R3, R5, R6, Ri8, R20, R21, R22, R23, R25, R26, R27 And R28 series hydrogen: 90038 -129- 19 200427680

I Compound No. B__ 442_O CF3 CF3_Lepidin-2-oxy compound of formula I, wherein A is CH to form a hexahydropyridine ring; n is 1, a single bond is formed from methyl charcoal (a) and its substituents; p, q, and r are 0; m and s are 1; B is a bridging group from methyl carbon to R; wherein R is pyridin-3-yl substituted with R17, R19, R2G, and R21; E is-(CR27R28 ) x- (CR29R3G) y- (where X is 1 and y is 0); and R8 is a phenyl substituted with R22, R23, R24, R25, and R26; where R1, R2, R3, R5, R6, R21, R22, R23, R25, R26, R27 and R28 series hydrogen: 19

R4 R5 I 90038 -130- 200427680

Compound number B R4

R 17

R 19 120

R 24 443 444 445 446 447 448 * Ri5 series hydrogen

0 CF3 H 0C (= 0) NR15 * CF3 h 〇C (= 0) NR 丨 5 CF3 h 0C (= 0) NR15 CF3 h 0C (= 0) NR15 CF3 Cl 〇C (= 0) NR 丨 5 CF3 HHH Cl CN H CF,

Cl HHHHH pyridine-2-oxypyridine-2-oxypyridine-2-oxypyridine winteroxypyridine-2-oxypyridine-2-oxy compound of formula I, wherein A is CH, forming a hexahydro p ratio Lake ring; with system 1, a single bond is formed from methyl stone trans (a) and its substituent; p, q &amp; r system 0; s system 1; b is a bridging group from methyl carbon to R; where r is Pyridin-4-yl substituted with Ri7, R18, R2O &amp;R2l; E-series-(CR27R28) x_ (CR29R3〇) y- (where X is 1 and 乂 0); and R8 is R22, R23 , R24, R25 &amp; R26 substituted phenyl; R1, r2, R3, R5, R6, Rl7, r21, r22, r23, R25, R26, r27 and r28 are

I Compound No. B R4 R18 R20 R24 449 * 〇ocf3 HH 2-methyl-2H-tetrazol-5-yl 450 〇C (= 0) NR15 &quot; cf3 HH Ye Diandian-〗-oxy 451 〇C (= 0) NR15 cf3 Cl Cl N-oxide of the pyridin-2-oxy * pyridin-4-yl moiety ** R15 is a hydrogen 90038 -131-200427680 compound of formula I, in which A is CH, and the shop is now &amp; ^ 々 ^ 哫 pyridine ring; η system 1, a single bond is formed from methyl carbon (a) and its substituent; ρ, ^ Λ 1 ^ 疋 P q and r system 〇; m &amp; s system I; β From methyl carbon to R foot bridge; where R is substituted with Ri9, R2〇 and substituted Da Geng-m; Ei (ci ^ r2V (cr29r3v (m_m_ ^ r8

R R25, R26, R27 and R28 are hydrogen phenyl groups substituted with R22, R23, R24, 1 ^ and r26; of which r1, r2, r3, R5, R6, R20, R21, R22 n 19

———- 5_〇CF3 Cl 2-methyl-2H-tetrazol-5-yl compound of formula I, wherein A is CH to form a hexahydropyridine ring; 丨, from methyl prostitute (a) and its substituents Formation of single bond; p, q &amp; r system 0; ^ and 5 system 1; b system as bridging group from methyl carbon to R; wherein phenyl system substituted by ruler system, R18, R19, R20 and R2i; E system-( CRnR, x_ (CR29R3V (where is 0), and R8 are phenyl substituted with R22, R23, R24, R25 &amp;R26; where R1, R2, R3, R6, R21, R22, r23 'r25, r26, r27 and r28 series hydrogen: 90038 -132- 200427680

R4 R5 I

90038 -133-200427680 4M 455 456 457 払 58 459 Ren 60 払 61 払 62 払 63 Carry 64 払 65 払 66 § Ren 68 i Ren 70 Ren 71 払 72 Ren 73 払 74 払 75 厶 76 OO0000¾00 (卩 0) 2 Acupoint ocno) NR 00 (卩 o) MH ocxhconh ocno) NR on? W§- ochonr. ocllo) NR ⑺ ocllo) NR. ocno) NR a) ocnCONRc; oclro) NR. ocno) NR = ocno) NR. oc (ho) nr-) oclro) NR. oc (ho) nr. OCIIONR ocho) nr 15 15 15

! H / H CF3 / HH / H OF3 / H! H / H CF3 / HH / H CF3 / HIH / H OCF3 / HH / H CF3 / H! H / H CF3 / HH / H Mi002cffi (CH3) 2 / ffi H / j H / H OCF3 / HH / HF / HH /! H / H OCF3 / HH / HF / HH / 丨 H / H OCF3 / HH / FH / FH / 丨 H / H OCF3 / HH / FH / F HA -H / H OCF3 / HH / FH / FH / — H / H CF3 / HH / H Cl / H Hz— H / H CIVH H / FH / FH / ι H / H CFVH H / H Cl / H HA, H / H CF3 / HH / FH / FH / ι H / H CF3 / HH / FH / FH / — H / H OCF3 / HH / HF / H Η / ί H / H OCF3 / HH / FH / FH / — H / H Cl / HH / H Cl / HH / ι H / H Cl / HH / HF / HH / 丨 丨 H / H Ol / HH / CF3 H / HH / 丨 H / H Cl / HH / H CF3 / HH / — H / H Cl / HH / FH / FH / — H / HF / HH / H Cl / HH / ι H / HF / HH / HF / H OHH ^ on2H5 ^ Λ · 2-^^ &gt; ^^-2- ^^ Mffi002CH (cffi3) 2 KQ Cl F Ioffi §¾¾ 2; H2 C5H-100¾〇ΠΗ3 OC3K7 OC3S7 OC3H7 OC3H7 OC3H7 OC3H7 OC3H7 Β

R-VRS RV ^ RVR- R 「/ R 一-

Rs / Rg

R 24 90038 -134- 200427680

All Ren 78 Ren 79 Private 80 Private 81 482 矣 3 矣 4 Ren 85 矣 6 Private 87 4-88 矣 9 490 Ren 91 492 493 払 94 4-95 払 96 Ren 97 払 98 499 500 ocllo) NR ^ ocho) nr ^ oclro) NR. oc (ho) nr. oclro) NR = 00 (HO) N1R ^ ocho) nr. on ^ nno ^^ oc (ho) nr ^ ocito) nr3; ocno) NR = ocno) NRc: oc (HO) NRe; oclro) NR3; oclro) NR = oo ^ now ^^ 00¾¾ ^ oclro) NRc; ocnozR. oclro) NR two oo (ho) nr- ocllo) NR a -ocllo) NR ^ ochonr. H / 丨 丨 H / —— H / 丨 丨 H / 丨 丨 H / 丨 丨 HA-HA · H /! H / 丨 丨 H / ι H / 丨 — H / 丨 丨 H / 丨 丨 H /! H /! H / 丨 丨 HA- Η / ί H / 丨 丨 H / 丨 丨 H / 丨 丨 H / 丨 丨 H / 丨 丨 H / 丨 丨

H / HH / HH / HH / Cl H / Cl H / Cl H / Cl H / Cl h§3 H, CF3 H, CF3 H / CF3 H / CF3 H / HH / EH / HH / HH / HH / HH / HH / H _ H / HH / H

F / HF / HF / H Cl / H Cl / H Cl / H Cl / H Cl / HH / HH / H _ H / HH / H CF3 / H CFs / H CF3 / H CF3 / H CF3 / H CF3, H CF3 / H CF, H OF3 / ffi CF3 / H Cl / H

H / CF3 _ H / FH / HH / HH / FH / CF3 H / HH / H m / HH / FH / CF3 H / HH / HH / FH / HH / FH / HH / FH / FH / FH / FH / FH / HH / H CF3, HH / F Cl / HF / HH / FH / H CF3, H Cl / HF / HH / FH / H CF3, Ha / s ffi / F a / ffi H / Fcl / ffi H / FE / FH / FH / FH / F c§ OC3K7 83H7 OCK7 OCS7 0PH7 OS7 R3H7 OC3K7 83H7 83H7 83H7 0PH7 OC3H7 0PH7 83H7 n02CH (CH3) 2 002CH (CH3) 2 NHCHO0H3 NHCn0nH3CH3Cr0) NH002CH3 MH002C2H5 NHC02CH (CH3) 2 Β R one VR one. RV ^ RVR)

R`` / RS

R3 / RS

R 24 90038 -135- 200427680 501 502 503 504 505 506 507 508 509 510 511 512 513 514 515 516 517 518 519 520 521 522 523 523 524

oc (no) NR. oc (no) NR = oc (&quot; o) NR Two OO ^ HOWZ ^^ oc (no) NR. oc (&quot; o) NR a) ocno) NRr- oclrCONR ^ ocllo) NR ^ oclro) NR. oc (&quot; o) NR. ocno) NR = oclro) NR ^ oc (no) NR. ocno) NRc; ocno) NR = oc (ho) nr = oc (no) NR = ociro) NR = ocllo) NR ^ oc (&quot; o) NR onllo) NR 15 R ;! H /! H /! HA- HA-HA— H /! H / 丨 丨 H /! H / 丨 丨 Hz! H / 丨 — H / 丨 — H / 丨 丨 H / 丨 H / 丨 H &gt; _ H / 丨 丨 H / 丨 丨H / 丨 丨 H / 丨 丨 H / 丨 丨 H / ffi H / HH / HH / HH / H Cl / H Cl / HH / Cl H / Cl H / Cl E / HH / H _ H / HH / HH / HH / HH / HH / HH / HH / HH / HH / HH / ffi ns Cl / HF / HF / HF / H Cl / H Cl / HH / Cl H / Cl H / Cl S / H CF3, H OCF3 / H OCF3 / H 8F3 / H CF3 / H CF3 / H CF3, H CF3 / H CF3 / H CF3 / H CF3 / HQ / H α / 1-1

ffi / F H / F H / H H / F H / F H / H H / F H / H H / F H / F H / H H / F H / H H / F H / F H / F H / F H / F H / F H / F H / H H / F H / H H / F

H / HH / F Cl / HH / HH / F Cl / HH / F Cl / HH / HH / F Cl / HH / F Cl / HH / HH / FH / FH / FH / FH / FH / FH / HH / F Cl / HH / H 2Kn02CH (CH3) 2 NH002CH (CH3) 2 Nnn02CH (CH3) 2 NHn02CH (CH3) 2 NHn02CH (CH3) 2Zffi002cffi (nii3) 2 NH002CH (CH3) 2 2Hn02CH (CH3) 22ffino2nH; (offi3) 2NH cffi3) 2 2K002nffi (nffi3) N) zffin02CH (CH3) 2 Nffin02CH (CH3) 2 2H002CH (CH3) 2 N (吴 硌 -2-AXC02CH3) MffinH0) NHC2H5 2ffinlls) NHC2H5 NHClr0) N (CH3) 2 NHClro) NP ( o) (oc2H5) 2 onlro) NHOH3 0C (= 0) NHCH3 CSHNOC2H5 OH = NOn2H5 Β

^ 15¾ Ρ2Θ3 ρ4 / ρ5 R-7 / rIS R-0 / ¾ ▼ 24 90038 -136- 200427680 525 526 527 528 529 530 531 532 533 53 Private 535 536 537 538 539 540 541 542 543 544 545 545 546 547 548 oclro) NR oc (&quot; o) NR OO ^ HOW ^ ocho) nr 00¾¾ oclro) NR 00 (= 0) 211 oclro) NR oclro) NR ocho) nr OOC-COMR oo (HO) 2n ocno) NH 000-0) 211 oc (ho) nr οο (ηο) 2; π oclro) NR oo (no) 2R 00 ^ 0¾ oclro) NR oc (ho) nr = ocnoNR. oclro) NR. oclro) NR. Β K / 丨 -H / 丨 丨 H / 丨 丨 Η / ί H / 丨 · H / 丨 · H / 丨 丨 Η / «丨 H / 丨 Η / 丨 丨 H / 丨 丨 0κ3 /! H / 丨丨 Η / ί Η /. 丨 H / 丨 丨 Η /. 丨 H / 丨 丨 H / 丨 H / 丨 丨 / 丨 丨 H / 丨 H / 丨 H / 丨 丨 Η / Η Η / Η Η / Η Η / Η C1 / H C1 / H C1 / HH / C1 H / C1 H / C1 Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η

Q / Ι-ί F / HF / HF / H C1 / H C1 / H C1 / HH / C1 H / C1 H / C1 CIVH CFVH OCF3 / H OCF3 / H 0F3 / H CF, H CF3 / H Q3 / H CF3 / H CF3 / H 0F3 / H CF3 / H CF3 / H CIVH

H / F Η / Η K / FH / F Η / Η H / FH / FH / HH / FH / FH / FH / HH / HH / FH / HH / FH / F ffi / FH / HH / FH / HH / FH / FH / FR】 VRS rm / ^ rvru R3 / R…

H / F Cl / HH / HH / F Cl / HH / HH / F Cl / HH / HH / FH / HH / H Cl / HH / F Cl / HH / FH / FH / F Cl / HH / F Cl / HH / FH / FH / F CHHNOC2H5 nffiHNOC2H5 nH = NOn2H5 OHHNOC2H5 cffi = NOC2H5 CKHNOC2H5 cffi = NOC2n5 CKHNOn2ffi5 nHHNOC2 OP- (2) # (2) Η2 2 6 丨 F2-ph)

R 24 90038 -137- 200427680 549 550 551 552 553 5M 555 556 557 558 559 560 561 562 563 564 565 566 567 568 569 569 570 571 572 573 oc (= o) NR on (卩 0) ¾ ^ 00 (卩 o) ZR οηΎΟ ^ 00 (卩 0) 211 ocllo) NR 00 ^ 0¾ ΟΟΎΟ ^ oo (&quot; o) NR oc (ho) nr oclroNR. oclro) NR = ocno) NR ^ oclro) NR. oclro) NR. oc (ho) nr3; oc (= o) NR. oclio) NR. ocno) NR. oclro) NR = ocno) NR. oclro) NR One. oc (&quot; o) NR. oclro) NR ^ oc (ho) nr ^ 15 15 15 H! HA-HA-H / 丨 丨 H / 丨 丨 H / 丨 丨 H / 丨 丨 H / 丨 丨 H / 丨 丨 H / 丨 — H / 丨丨 H / 丨 丨 H / 丨 丨 H / 丨 — H / 丨 丨 HA 丨 H / 丨 丨? 丨 Η / 丨 丨 H / 丨 H / 丨 丨 H / 丨 Η /! ΜΑΗ / 丨 — _ Η / Η Η / Η Η / Η Η / Η Η / Η _ Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η H / H Η / Η Η / Η C1 / H C1 / H C1 / H C1 / H C1 / HH / C1 H / C1

CF3, H CF3, H CF3, H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3, H 0F3 / H Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η C1 / H C1 / HH / FH / FH / FH / FH / FH / F Η / Η H / F Η / Η H / F Η / Η H / F Η / Η H / FH / F _ Η / Η H / CF3 Η / Η H / C1 H / FH / F Η / Η Η / Η H / C1

H / FH / FH / FH / FH / FH / FF / HH / FF / HH / FF / HH / F 01m H / FE / F Cl / H CF3 / HH / Fα / κ Cl / HF / HH / F CF3 / HQ / K Cl / H 0nH2ph NHClr0) (2.crph) NHCH0) (2,6-C12, ph) NHOno) (2,6_Frph) NHCH0) (20CH3-ph) NHCll0) (40CHrph) s-^-r ^ ^ Tik. 丨 1 丨 ^ &gt; l, 2 &gt; w ^ -r; &amp; 3 丨 crlNJv ^ l · ^-^^ 1,3-Chizao, 2-¾ 漭 _ 2 丨 o ^ -2H, s ^ -5 丨 One: 2 丨 ^ 2-6 ^ -2H-s ^, 5-_ 2-6ά-2Η · β ^ -5 丨; &amp; 2-6i-2H-Q ^ .5i; &amp; 2-6w &gt; -2H-s ^ -5 丨; &amp; 2 丨 6 ^ -2H-s ^ -5 丨 蝌 2-ο ^ · 2Η-3 ^ -5 丨 One: 2-c ^^-2H- s ^ ~ 5 丨, 1t fate β Β ^ 1¾ rv ^ rvrm r】 vrs 5¾

R 24 90038 -138- 200427680 574 575 576 577 578 579 580 581 582 583 584 585 586 587 588 589 590 591 592 593 5 9 払 595 596 597 598 on (卩 C02H on (HO) MR oochconh ocno) NR oc (= o) NR 000 = 0) 2 ^ 00 (卩 0) 211 ochonr 00 (= 0) 211 οηΎΟ ^ 00 (卩 0) 211 oclro) NR 00 (= 0) 2R oo ^ now ^ oc (&quot; o) NR 000 = 0) 211 oclrozR 00 (= 0) 211 00 (= 0) 211 ocno) NR oclro) NR oclio) NR oo (ho) 2r 00 (卩 0) 2R ocxhcomu Β Η / ί H /!? «H /丨 丨 H / 丨 H / 丨 丨 H / 丨 Η / ί H / 丨 HA-HA-H / 丨 丨 HA-HA-HA-H /! H /! H / — H / 丨 — H / 丨 丨 H / 丨 H / — H /! H / l H /!

H / Cl H / Cl H / Cl H / Cl H / Cl H / Cl H / Cl H / Cl H / FH / FH / FK / FH / FH / F ffi / FH / FH / F ffi / FH / FH / FH / FH / H _ H / HH / H

Cl / H Cl / H Cl / HH / Cl H / Cl H / Cl H / Cl H / QH / HH / HH / HH / HH / HH / HF / HF / H ffi / FH / FH / FH / FH / F CH3 / H CH3 / H CH3 / H OHVH R】 VR5 RV ^ RVR-

H / F ffi / FH / HH / HH / Cl H / FH / FH / HH / HH / Cl H / FH / FH / 0F3 H / H _ H / FH / HH / Cl H / FH / FH / H _ H / Cl H / FH / F

F / HH / F CF3 / H 01 / ffi Cl / HF / HH / F CF3 / H Cl / H Ol / HF / HH / FH / H CF3 / H Cl / HH / FQ / n Cl / HF / HH / F Q3 / HQm Q / KF / HH / F

2 丨 丨 2ffi 2 丨 π; &amp; ι2Η 2 丨 π ^ ΜΗ 2 · 6 * —2Η 2 丨 ^ _ 丨 211 2 丨 2 丨 6; &amp; 丨 2Η 丨 2Η 2 · 6α · 2η 2 丨 6; &amp; 丨 2Η 2 丨 6 ^ -2η 2- £ -2Η 2 丨 6 丨 2Η 2 丨 π ^ &gt; 丨 2H 2 丨 £ 丨 2Η 2 丨 £ · 2Η 2 · π ^ &gt; 丨 2Η 2-6 *- 2Η 2 丨 2 丨 2-6w &gt; —2H 2 丨 丨 2H s ^-5 丨; One: 3 ^ -5- ^ s ^-5_ ^ 3 ^ -5—is ^ -5- ^ s ^- 5-w &gt; 3 ^-5- ^ s ^ -5- ^ 3 ^ -5- ^ 3 ^ -5-¾ s ^-5- ^ 3 ^ -5-: ¾. 3 ^ -5- ^ 3 ^-5- ^ s ^ -5- ^ 3 ^ -5- ^ s ^ -5- ^ 3 ^ -5-: 1: • s ^ -5-: sl —Q ^ -5 丨 _ ρπ / ^ s

R3 / R 20 -24 90038 -139- 200427680 599 600 601 602 603 62 605 606 607 608 609 610 611 612 613 614 615 616 617 618 619 620 621 622 S3 ** oc (= o) MFl = ocno) NR. oclro) NR. ocno) NR-ocno) NR. oc (no) NR-oc (&quot; o) NR ^ oc (no) NR. oclro) NR. ocno) NR. ocno) NRe ^ oclro) NRc; oc (&quot; o) NR a) ocnoNR. ocno) NR. oc (ho) nrc ^ ocllo) NR]) oclro) NR = ocno) NR = ocllo) NR. oclro) NR. oclro) NRr-oc (&quot; o) NR = oclro) NR. H / — 丨 H / 丨 丨 H / 丨 丨 H / — H / 丨 丨 H / 丨 H /! HA 丨 H / 丨 丨 H / — H / 丨 丨 HA-HA-HA-H /! HA-HA -H /!? «H / 丨 H /! H / 丨 丨 H / 丨 H / 丨 丨 H / 丨 丨 H / HH / HH / HH / HH / HH / HK / HH / HH / HH / onK H / OS3 H / HH / HH / HH / HH / HH / HH / HH / HH / HH / HH / HH / H _ H /!

OH3 / H OH3 / H OOHb / H OS3 / H OOK3 / H OCH3 / H OOHb / H 8H3 / H OS3 / H OOH3 / H OOK3 / H OF3 / H IPh / H Ph / H Ph / H IWH 弋 h / H OPh / H OPh / H OJPh / H OPh / H OPh / H OPh / H OPh / H 丨 丨 / H

H / CF3 H / HH / HH / Cl E / FH / FH / 0F3 H / HH / HH / HH / FH / FH / HH / Cl H / FH / F _ H / HH / Cl H / FH / FH / CF3 H / HH / HH / H

H / H Q3 / Hc§ Cl / HF / HH / FH / H CF3 / H Ph / H Cl / HH / FK / F Cl / H Cl / HF / H _ CF3 / H Cl / HQ / HF / HH / FH / H Ph / H OPh / H Cl / H 2 丨 ^ 丨; &amp;2-6; sl-2h-s ^ -5— ^ 2-6 ^ -2h-s ^ -5-; &amp; 2lc ^^ -2H-s ^ ~ 5- ^ 2-c ^^-2H-s ^ -5 ~ ^ 2 丨 C ^^-2H-s ^-~ 5 丨 Office 2 丨 ^ i-2H-s ^ -5 丨_ 2 丨 c ^^-2H-s ^ -5- ^ 2 丨 c ^^-2H-s ^ -5- ^ 2-6 ^ -2H-s ^ -5 丨; &amp; 2-6 ^ -2h -3 ^ -5-1l 2—61l-2h-s ^ -5- ^ 2-o ^ -2H-s ^ -5 丨 a: 2—o_-2H-3 ^ -5 丨 唞 2 · 6 ^, 2η-3 ^ · 5-_ 2 丨 6; &amp; -2H-0 ^ -5 丨 Lion 2 丨 6_-2H-s ^ -5- ^ 2 丨 6; &amp; -2H-s ^ -5- ^ 2-6; sl-2h.s14-5- ^ 2-6i-2H-s ^ -5_ ^ 2—π ^ · 2Η-3 ^ -5 丨 _ 2-6, -2η-3 ^ -5-; &amp; 2 · 6; &amp; .2Η-β ^ · 5— ^ Β RV ^ RVR) R-VR-1

R3 / RS

R 24 90038 -140- 200427680 Jinming Rongweng Line 624 ** &lt; 525 ** S6 ** 627 628 629 630 631 632 633 634 635 S6 &lt; 537 638 639 640 6 death 642 § 644 645 646 § §

ο 〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇οοοο ^^ ηηηοοοοοηηηοηοοηο II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II II ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο Mt W »^ Ν- ^ Ik · ^ k—V-Mk Μ— ^» · »^ to-xA Μ P g;« -Λ Lyi tn Ol Cyi H / 丨 丨 H / 丨 丨Η / ί H / 丨 丨 HA 丨 H / 丨 丨 H / 丨 丨 H / 丨 H /-丨 H / 丨 丨 H / 丨 丨 H / 丨 丨 S3 / 丨 C2H5 /. · H / 丨 丨 Η / — H / 丨 H / 丨 丨 Η / 丨 丨? 丨 Η /! H / 丨 丨 H / 丨 丨 ΗΑ-Η / 丨 丨 // Η / Η _ Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η H / C1 H / C1 H / C1 H / C1 H / C1 Η / 丨 丨 Η / ί H / 丨 丨 Η / Η H / H Η / Η Η / Η Η / Η Η / Η Η / Η

丨 丨 / Η — 丨 / Η 丨 — / Η CF, H CF3, H C1 / Ham Cl / H Cl / H Cl / H Cl / H Cl / H Cl / Ha / H Cl / HF / HF / HF / HF / HF / Ha / ffi Cl / Ha / K Cl / H Cl / HH / Cl H / FH / FH / HH / FH / HH / HH / FH / 0H3 H / 0S3 H0F3 H / HH / HH / HH / 002CH3 H / H _ H / F HHF3 H / HH / HH / HH / HH / FH / OCK-

Q / n F / HH / F Cl / KH / F Cl / HF / HH / FH / 0H3 H / 0S3 H / H CF3 / H CF3 / H CF3 / HH / H Cl / HF / HH / FH / H Q3 / H CF3 / H Cl / HF / HH / FH / H 2-6; &amp; -2Η-0 ^ -5-1: 2-c ^^-2HIS ^ -5i ^ 2 丨 C ^^ l2H—3 ^- -5- ^ 矣 ^ -2 丨 _ 矣 ^ -2- ^ 吴 硌 -2- 烨; &amp; 奂 ^ -2- | 1 ^ ^-^-2 — ^^ Wuwei-2-tick; &amp; ^-^-2-^: 1: ^ Λ-2-^^ 奂 硌. 2-11¾ 矣 ^ -2-^^ 矣 ^ -2-^^ 矣 ^ -2-^^ ~ 2-^^ &gt; 矣 ^ -2-^^ s. ^ — 2-^^ ^-^-2-^^ Wu ^ -2-^^ 奂 硌 -2- ^ i 矣 ^ -2-, ^ ^-^ 12- ^^

Cd

R-VRS RVRW RVRW

R-VRS 5¾

R 24 90038 -141-200427680 649 650 651 652 653 654 655 656 657 658 659 660 661 662 663 664 665 666] 667 668 669 670 671 672 672 oclro) NR -nHRg oclro) NR -o ^ HRg 〇0 (&quot; ○) oc (no) NR = ocHo) NRe; CHR5; ocllo) NR. oc (&quot; o) NR. oc (ho) nr-on (卩 s) 2r3; oo (no) lNIl ^ so2 oclro) NR = oc (ho) nrc; oc (ho) nr. oc (&quot; o) NR. oclro) NR =

oc (ho) nr oc (= o) NR oclro) NR oclro) NR 00 (卩 0) 2R oc (ho) nr ^ oclro) NR. 00 ^ 0¾ oclro) NR 15 15 15 15 H / 丨 -H / —— H /! H / — Η / ί H / 丨 丨 H / 丨 — H / 丨 丨 H / 丨 丨 ffi 3 /! H / HH / 0H3 H /! H / HH / 丨 丨 H / 丨 — H / 丨 H / 丨 丨 HA-H / 丨 丨 H / 丨 H / 丨 丨 H / 丨 丨 H / 丨 丨

H / Cl H / Cl H / Cl H / CF3 H / CF3 H, CF3 H / CF3 H / CF3 H / HH / HH / HH / HH / H ffi / HH / HH / HH / HH / HH / HH / HH / HH / HH / HH / HH / H

cl / ffi Cl / H Cl / HH / HH / HH / HH / HH / H CF3 / H CF3 / HC ^ / H CF3 / H CF, H CF3 / H CF, H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H oivH

ffi / 00K3 H, CF3 H / HH / H m / HH / FH, CF3 H / HH / HH / HH / HH / HH / H Cl / H Cl / HH / Cl H / HH / HH / H ffi / HH / HH / HH / HH / Br H / H s / onl ^ H / H CF3 / HQ / KF / HH / FH / HH / HH / HH / HH / HH / HH / HH / ffi H / HQ / H Cl / H 01 / Ή Q / ffi Cl / H nl / ffi Cl / HH / H Br / ffi ^-^-2-¾ ^ ^^-2-¾ ^ f ^. ^-2-^^ 1 12- ^ 私 ^ ^ ~ 2- ^ w &gt; ^. ^-2-^^ 吴 硌 -2- # l; &amp; ^. ^-2-^^ ^^-2-¾ ^ s. ^-2-^^ Wu ^ —2-^^ s-^-2-^^ 矣 ^ -2-^^ Wu ^ -2-^^ Wu 硌 -2-IL ^ N-lub Match 3 丨 ^^^ Λ-2-^^ 5丨 ^^^^-2-^^ ^-^-2-^^ Fit to wear Μβ Β R one VR5 RVR- RVR-

R 24 90038 -142-200427680 674 675 676 677 678 679 680 681 682 683 684 685 686 687 688 689 690 691 692 693 6¾ 695 696 697 698 oclro) NR. ocno) NR = ocno) NR] nHRg on (卩 0)> ill ^ oc (HO) NR = CHRg oclro) NR. oc (&quot; o) NR. oc (卩 0¾¾ ocno) NR. oo (HO) 2R ^ oo (&quot; o) NR = oc (ho) nr. ocllo) NR = oo (ho) zr ^ ocllo) NR Two 00¾¾ ^ ocns) NR = oclls) NR. oc (ho) nr ^ chr3; oc (ho) nr-ecHRg 0n (H0) zjRG; s02 00 (卩 ο) Νηπ ocno) NR-nHRg Β ffi / 丨 H / 丨 丨 Η / ί Η / ί H / 丨丨 H / 丨 丨 Η / 丨 丨 Ε / ί ΗΑ 丨 H / 丨 H / 丨 丨 Η / 丨 丨 Η / 丨 丨 // 丨 丨 H / 丨 丨 Η / 丨 丨? «H / 丨 丨 Η / ί H / 丨 丨 H / 丨 丨 Η / 丨 丨 H / 丨 丨 H / 丨 丨 H / 丨 丨 Η / Η Η / Η Η / Η Η / Η Η / Η Κ / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η Η / Η

Q3 / H CF3 / H CIVH 0F3 / H CF3, H S3 / H CF, H CF3 / H CF3 / H CF3 / H CF, H CF3 / H Q3 / H CF, H CF, H CF3 / H 0F3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H CF3 / H

R ^ R; RV ^ RVRU

H / F _ Η / Η Η / Ηa / ffi WH H / FH / FH / FH / FH / FH / FH / FH / FH / FH / FH / FH / FH, CF3 H / HH / CK3 H / HH / HH / FH / H

R3 / RS

H / HF / HF / HI / H Cl / HF / HH / F _ H / FH / FH / FH / FH / FH / FH / FH / F ffi / FH / FH / H 0F3 / H _ 0H3 / H 0H3 / HF / FocffiVH s-^-2-^^ Wu ^ -2-^^ ^-^ 12- ^ 办 ^-^ • 2-IL; iL ^^-2-¾ ^ 奂 ^ -2- ^ 1: 3 -cl _ ^^. 2-ILi 5 丨 cl-^^-2 ~ ^^ 6-cl- ^ b ^ -2-^^ 3VC12- 奂 is -2-il ^ 3 丨 ^^ 矣 ^ -2- ^ ^ 5-^^^^-2-^^ 3-CFr Wu 硌 -2-Tick ^ 4 丨 CF3 · 吴 Λ 丨 2- ^ i 5 丨 CF3- 吴 硌 -2-lli ^-^ 12-^^ &gt; ^. ^ ~ 2-^^ s-^-2-^: sl s-^ — 2-^^ ^. ^-2-^^ R3 / Rg

R 24 90038 -143- 200427680 Democracy buds β699 701 700 701 702 703 72 705 706 707 708 709 710 ) NRe ^ ocno) NR-oclro) NR ^ οο (ηο) μιι ^ ocho) nr ^ oc (= o) NR. ocllo) NR = ocno) NR. on? w§-oc1lo) NR-⑺ ocllo) NR-) ocno) NR. oc (ho) nrc ^ ocho) nr ^ ocho) nr. oc (ho) nr. ocho) nrc: oc (ho) nr ^ oclro) NR】 a ocno) NR = oclro) NR = oc (no) NR = ociro) NR = Β

H / l H / H CF3 / H Η / Cl OCH3 / HH / — H / H CF3 / HH / F OOH3 / HH / 丨 H / H CF3 / HH / H OOHF2 / HH / 丨 H / H CF3 / HH / H SCH3 / H H &gt; 丨 H / H CF3 / HH / H SCF3 / H HA · H / H CFVH H / H δ / Η H / 丨 H / H CF3 / HH / H CIT00H3 / HH / — H / H OCF3 / HH / H Cl / HH / — H / H OCF3 / HH / H Cl / H?, H / H OCF3 / HH / H Cl / HH / j H / H OCF3 / HH / FH / FH / — H / H OCF3 / HH / FH / FH / — H / H OCF3 / HH / FH / F?, H / H Cl / HH / H Ol / HH / l H / H Cl / HH / FH / HH / l H / H Cl / HH / FH / FH / ι H / HF / HH / H Cl / HH / ι H / HF / HH / FH / HH / l H / HF / HH / FH / FH / — Ol / H Cl / HH / H Ol / H ffi / ί nl / H nl / u H / FH / HH / 丨 Cl / H Cl / HH / FH / F h /! Η / Cl Cl / HH / H Cl / HH / — Η / Cl Cl / HH / HF / HH / 丨 * Η / Cl Cl / HH / FH / FR-VRS RV ^ RVR-

R-VRS 矣 ^ -2-^^ ^-^ 12-^^ ^-^ 12- ^ Do 矣 —2- ^ w &gt; 矣 硌, 2-ll ^, N-lucv # 3 丨 ^^ 矣 ^ -2- ^ 办 5 丨 ^^^-^-2-^^ 奂 硌 -2-IL ^ N- # ub Reference 3 丨 ^^^ Λ—2 — ^^ 5 丨! Wu ^^-2-il, ^^-2-ilw &gt; ^^-2-^^ ^^-2- ^ ¾ ^^-2-^^ ^^-2-¾ ^ Miscellaneous ^ -2-il ^ »^ -2-^; sl ^^ &gt; -2-ϋ, ^» ^ -2-^^ ^^-2-^^ &gt; 24 90038 -144- 200427680 参 参 705 4sr ^ tc (&quot; o ) nhch3 * Mb life parameters 623, 624, 625 涔 Ί7A 725 726 727 728 729 730 731 732 733 733 734 735 736 737 738 739 740 oc (no) NR3; ocnoNR. ocho) nrg; oclro) NR. ocllo) NR-- on (HO) zn3; oclro) NR ^ ocllo) NR. ocno) NRe ^ oclro) NRe; oclro) NR ^ oclro) NRC oclro) NR ^ 0C1I0) NR. oclro) NR = ocno) NR ^ Β H / 丨 H /! Ii / 丨 丨 H / 丨 H / — H /! H / 丨 丨 H / 丨 Η / ί Η / ί H /. 丨 HA 丨 H / 丨丨 Η /! H / 丨 丨 H / ι H / 丨 丨 626: Yellow ^; 5L ^^-CHAHCHncH'5i ^ ί Full.

Η / Cl Η / Cl H / Cl H / Cl H / Cl Ή / Η H / H H / H H / H H / H H / H H / K H / H H / H H / H H / H H / H

Cl / HQ / KH / Cl H / Cl H / Cl CF3 / H CF3 / H CF, H CF3 / H OCF3 / H OCF3 / H OCF3 / H CF3 / HS / H CF3, H CF3 / H CFVH R] VRS RV ^ RVR-

H / OF3 H / H H / H H / F H / F H / H F / H ffi / F H / F _ H / F H / F H / F H / H H / F H / F H / F

H / H CF3 / H Cl / HH / HH / FQ / ffi F / HH / FF / H Cl / HH / HH / FH / F Cl / HH / FH / FH / F ^^-2- ^ ¾ ^^, 2- ^ ¾ ^^, 2-¾¾ ^^-2-IL ^ ^^ 12--¾ ^ ^^-2- ^ ¾ 麻 手 3—, ^ 6 丨 羚 ά / 4ι · 3 · ^ &amp; 6丨 羚 ilacid · 3 · # ι ^ Uvw, r2-IL; 1L 4,6 · &quot; όαί3,1,3νΗ ^ 丨 2 丨 ^

Rs / Rg

R 24 90038 -145-200427680 Compounds of formula I, in which human is CH, carbon (a) and its substituents form a single bond to form six bonds, and d is bad; η is 1, from methyl 'ρ is 0; m And S series 1; B is a bridging group from methyl carbon to R; wherein R is a phenyl group substituted with R18, r19, R20, and R2i, q is 0 and r is 1, forming an N-oxide; E is -(CR27r28) x, (CR29R3〇) y_ (where X is 1 and y is 0); and R8 is phenyl substituted with R22, r23, r24, Rh, and R26; of which R1, R2, R3, R5, R6 , R21, R22, R23

R 25

R 26 R27 and R28 series hydrogen: 19

90038 -146- 200427680 Compound No. B R4 R17 / R18 R19 / R20 R24 741 0C (= 0) NRi5 * cf3 H / FH / F OC3H7 742 〇C (= 0) NR15 cf3 H / FH / H ch = n〇c2h5 743 0C (= 0) NR15 cf3 H / FH / F ch = noc2h5 744 0C (= 0) NRi5 cf3 H / FH / F ch = noch2c = ch 745 0C (= 0) NR15 cf3 H / H Cl / H c. 2ch (ch3) 2 746 0C (= 0) NR15 cf3 H / FH / F nhco2ch (ch3) 2 747 〇C (= 〇) NRi5 cf3 H / H Cl / H Ph 748 〇C (= 〇) NR15 cf3 H / FH / F Ph 749 0C (= 0) NR15 cf3 H / FH / F OPh 750 0C (= 0) NR15 cf3 H / FH / F 0 (2-F-Ph) 751 0C (= 0) NR15 cf3 H / FH / F 0 (2,6-FrPh) 752 0C (= 0) NR15 FH / FH / F Outer Dian-2-oxy 753 0C (= 0) NR15 cf3 F / HF / H 17 754 0C (= 0) NR15 cf3 H / FF / H p ratio lake 2-oxy755 OC (= 〇) NR15 cf3 H / FH / F 3-chloropyridine-2-oxy756 OC (= 〇 ) NR15 cf3 H / FH / F 5-aminopyridine-2-oxy 757 0C (= 0) NR15 cf3 H / FH / F 6-chloropyridine-2-oxy758 〇C (= 0) NR15 cf3 H / FH / F 3,5-di-Cl2-pyridine-2-oxy 759 0C (= 0) NR15 cf3 H / FH / F 3 &lt; cardiopyridine-2-oxy760 0C (= 0) NR15 cf3 H / FH / F 4-CF3-P ratio Yodo-2-oxy761 〇C (K)) NR15 cf3 H / FH / F N- (methoxycarbonyl h ratio pyridine-2- Amino 762 oc (o) nri5 cf3 H / H Cl / H 763 0C (-0) NR15 cf3 F / HF / H 13 dense lake 2-oxyl 764 0C (-0) NR15 cf3 H / FF / H p dense lake 2-oxy 765 0C (= 0) NR15 cf3 H / FH / F pyrimidine-2-oxy 766 〇〇cf3 H / H cf3 / hp dense lake 2-oxy 767 0C (= 0 ) NR15 cf3 H / H Cl / H 6-Aminopyridin-3-yl 768 OC (= 〇) NR15 CF3 H / F * R15-based hydrogen H / F 6- in compounds 741-765, 767, 768 Chloropyridin-3-yl 90038 -147-200427680 Compounds of formula I, in which the eight-chain CH forms a hexahydropyridine ring; the η-series 1, forms a single bond from methyl carbon (a) and its substituents; p, q And r are 0; m and s are 1; B is a bridging group from methyl carbon to R; E is-(CR27R28) x- (CR29R3Q) y- (where X is 1 and y is 0); and R8 is Phenyl substituted with R22, R23, R24, R25 and R26; wherein R1, R2, R3, R5, R6, R22, R23, R25, R26, R27 &amp; R28 are hydrogen:

Compound B R15 R16 R R4 R24 No. 769 〇—…-CH2CH = CH cf3 leaf alkoxy 770 0C (= 0) 0 — ——- CH (CH3) 2 cf3 leaf dike-2-oxy771 0C (- 0) NR15 H…-ch3 cf3 pyridyloxy 772 OC (= S) NR15 H…-ch3 cf3 p ratio lake-2-milk 773 0C (= 0) NR15 ch3-ch3 cf3 ch = noc2h5 774 0C (= 0) NR15 H C2H5 cf3 outer dagger -2-oxy775 〇C (two 0) NR15 H…-C3H7 cf3 leaf dagger-〖-oxy 776 0C (= 0) NR15 H ----- ch (ch3 ) 2 cf3 Outer Dykeline-2-oxy777 OC (= S) NR15 H… · CH (CH3) 2 cf3 ^ Biyodo-2-oxy778 〇C (= 〇) NR15 ch3 -... CH (CH3) 2 cf3 pyridine-2-oxy 779 〇C (= 〇) NR15 H ---- C (CH3) 3 cf3 p ratio lake 2-oxy 90038 -148- 200427680 compound number BR 丨 5 R16 R R4 R24 780 0C (= 0) NR15 H — ch2ch = ch cf3 pyridine-2-oxy 781 0C (= 0) NR15 H — cyclopentyl cf3 pyridine-2-oxy 782 0C (= 0) NR15 H — cyclohexyl cf3 pyridine -2-oxy783 0C (-0) NR15CHR16 HH CO2C2H5 cf3 pyridine-2-oxy784 0c (= o) nr15chr16 H CH (CH3) 2: c09ch3 cf3 pyridine-2-oxy compound of formula I, Where A is CH and forms a hexahydropyridine ring; n is 1 Form a single bond from methyl carbon (a) and its substituents; p is 0; m and s are 1; B is a bridging group from methyl carbon to R; q is 0 and r is N-oxide; HKCR27R28) x- (CR29R30) plant (where X is 1 and y is 0); and R8 is phenyl substituted with Ru, ru, R24, r25 and R26; of which Ri, R2, R3, R5, r6, R22, r23, R25, R26, R27 and R28 series hydrogen:

R23 Compound No._B_R15 R R4__R24 785 OC (-Q) NR15 H CH (CH,) 2 CF3 Pyridine-2-oxy compound of formula I, in which A is C and forms a 1,2,5,6-tetrahydrogen ratio Benzyl ring; n is 1, forming a single bond from methyl carbon (a) and its substituent; p, q and r are 0; m and s are 1; B is a bridging group from methyl carbon to R; E System- (CR27R28) X- (CR29R3G) (X-series 1 and y-series in 90038-149-200427680); 118 series phenyl substituted with R22, r23, R24, R25 &amp;r26; and R series with R17, Rls, R19, r2 (^ r2i substituted phenyl; R1, R2, R3, R5, R6, R21, R22, r23, r25, r26, r27 and r28 are argon:

A hydrogen compound of formula 1 'wherein the eight series of 0' form a 1,2,5,6-tetrahydropyridyl ring; System 1, which forms a single bond from methyl ^ (a) and its substituents; p is 0; ^ and is 丨; B is a bridging group from fluorenyl carbon to R; q is 0 and r is 1, forming N-oxide; E-based-(CR27R28) x- (CR29R30) y- (where X is 1 and y is 0); R8 is phenyl substituted with R22, R23, R24, R25 and R26; and R is based on R17, R18, R19, R2. And R21 substituted phenyl; Ri, R2, R3, R5, r6, R2i, R23, R25, R26, R27 and R28 are hydrogen: 90038 -150- 200427680

Compound number B_R4 R17 / R18 R19 / R2Q__ 787 0C (= 0) NR15 * CF3 H / FH / F pyrimidine-2-oxy * R15 is hydrogen_ Compound of formula I, wherein A is C and forms a hexahydropyridine ring; m , P, q, and r are 0; s is 1; η is 0; a double bond is formed between the methyl carbon (a) and the 4-position of the hexahydropyridine ring; E- (CR27R28) x- (CR29R3G) y- (where X is 1 and y is 0); R8 is phenyl substituted with R22, R23, R24, R25 and R26; B is R9, R1. , R11,

Ri2 and Rn substituted phenyl; wherein R2, R5, R6, R9, Ri2, R13, R22, R23, R25, R26, R27 and R28 are hydrogen; R24

Rn 90038 -151-200427680 Compound number r2 / r3 / r4 / r5 R10 / R &quot; R24 788 h / h / cf3 / h H / CF3 〇c (= o) ch3 789 H / H / Cl / HH / Cl 0C ( = 0) NHCH3 790 h / h / cf3 / h H / CF3 0C (= 0) NHCH3 791 H / H / OCF3 / HH / OCF3 0C (= 0) NHCH3 792 H / H / CF3 / HH / CF3 0C (= 0) NHCH (CH3) 2 793 H / H / H / HH / H NHC02CH (CH3) 2 794 H / H / F / HH / F NHC02CH (CH3) 2 795 H / C1 / C1 / H Cl / Cl NHC02CH ( CH3) 2 796 H / F / Cl / HF / Cl NHC02CH (CH3) 2 797 H / H / CF3 / HH / CF3 nhc〇2ch2c = ch2 798 H / H / Cl / HH / Cl nhco2ch2ochch3 799 H / H / CF3 / HH / CF3 nhco2ch2c = chch3 800 H / H / Cl / HH / Cl nhco2ch2c (ch3) ch2 801 H / H / Cl / HH / Cl nhco2ch2c = ch 802 H / H / CF3 / HH / CF3 nhco2ch2c = ch 803 H / H / CF3 / HH / CF3 〇s〇2ch3 804 H / H / CF3 / HH / CF3 〇s〇2ch (ch3) 2 805 H / H / CF3 / HH / CF3 nhso2ch3 806 H / H / CF3 / HH / CF3 0 (2-F-Ph) 807 H / H / CF3 / HH / CF3 p ratio 2-yl 808 H / H / H / HH / H pyridine-2-oxy 809 H / H / Cl / HH / Cl Leaf Dike-2-oxy810 H / H / F / HH / F Leaf Dike-2-oxy811 H / H / CF3 / HH / CF3 Pyridin-2-ylamino 812 H / H / Cl / HH / Cl p dense lake 2-oxyl 813 H / C1 / C1 / H Cl / Cl shout lake 2-oxyl 814 Cl / H / H / HH / CF3 p dense lake 2- 815 H / Cl / H / HH / CF3 p dense lake 2-oxy 816 H / H / Cl / HH / CF3 oxo lake 2-oxy 817 H / F / H / H / H / CF3 2-oxyl 818 H / C1 / C1 / HH / CF3 p dense lake 2-oxyl 90038 -152- 200427680 24 compound number r2 / r3 / r4 / r5 10m π R ^ / R 819 H / C1 / H / C1 H / CF3 820 H / F / H / FH / CF3 821 H / F / C1 / HH / CF3 822 h / cf3 / h / h H / CF3 823 H / H / CF3 / HH / CF3 824 H / H / CF3 / HH / CF3 825 H / H / CF3 / HH / CF3 826 H / H / CF3 / HH / CF3

R bite-2-oxypyrimidine-2-oxypeptide-2-oxypyrimidine-2-oxy 3,4,5,6-tetrahydropyrimidine-2-oxypyran-2-oxo Pyridoxin-2-oxy ^ A chloropyridin-3-oxy formula 'wherein A series C' forms a hexahydroton ring; s series ι; η series 〇; A double bond is formed between the 4_ positions of the pyridine ring; the tear system 0; the q system 0 and r system form an N-oxide; the e system-(CR27R28) x ^ CR29R3〇) y- (wherein X system 1 and y system 〇); R8 is a phenyl group substituted with R22, R23, R24, R25, and R26; B is a phenyl group substituted with R9, R10, Ru, R12, and R13; where r6,

R9, R12, R 13

R 22 R23, R25, R26, R27 and R28 are hydrogen; R24

I 90038 153- 200427680 Compound number r2 / r3 / r4 / r5 R10 / Rl 丨 R24 827 H / H / C1 / HH / Cl 0C (= 0) NHCH3 828 H / H / CF3 / HH / CF3 0C (= 0) NHCH3 829 H / H / OCF3 / HH / OCF3 0C (= 0) NHCH3 830 H / H / CF3 / HH / CF3 〇c (o) nhch (ch3) 2 831 H / H / C1 / HH / Cl nhc〇2ch (ch3) 2 832 H / H / F / HH / F NHC02CH (CH3) 2 833 H / C1 / C1 / H Cl / Cl NHC02CH (CH3) 2 834 H / F / C1 / HF / Cl NHC02CH (CH3) 2 835 H / H / OCH3 / HH / OCH3 NHC02CH (CH3) 2 836 H / H / CF3 / HH / CF3 nhco2ch2ch = ch2 837 H / H / CF3 / HH / CF3 nhc〇2ch2ch = chch3 838 H / H / CF3 / HH / CF3 nhco2ch2c = ch 839 H / H / CF3 / HH / CF3 0 (2-F-Ph) 840 H / H / CF3 / HH / CF3 Leaf Dike-2-yl 841 H / H / C1 / HH / Cl Pyridine-2-oxy 842 H / H / F / HH / F Outer hydrazine-2-oxy 843 H / H / CF3 / HH / CF3 Ye Diandian-2 -ylamino 844 H / H / Cl / HH / Cl p dense lake 2-oxy 845 Cl / H / H / HH / CF3 pyrimidine-2-oxy 846 H / Cl / H / HH / CF3 p dense lake 2-oxy 847 H / H / Cl / HH / CF3 Hyoden-2-oxyl 848 H / F / H / HH / CF3 ρ Myodo-2-oxyl 849 H / C1 / C1 / H Cl / Cl ρ Myodo-2-oxyl 850 H / C1 / C1 / HH / CF3 ρ dense lake 2-oxyl 851 H / C1 / H / C1 H / CF3 shout lake 2-oxyl 852 H / F / Cl / HH / CF3 Xiangdian-2 -Oxy 853 H / CF3 / H / HH / CF3 ρ dense lake 2-oxyl 854 H / H / CF3 / HH / CF3 ρ dense lake 2-oxyl 855 H / H / CF3 / HH / CF3 6-chloro σ dahu-3-oxy compound of formula I, in which A is C and forms a hexahydropyridine ring; s is 1; n is 0; at 90038 -154- 200427680 the methyl carbon (&amp; Double bonds are formed between the 4_ positions; m and p are 0; q is 0 and r are 1, and j is turned into N-oxide; £ _ (cR27R28) x- (CR29R30) y- (where X is 1 and y is 0); R8 is phenyl substituted with R22, r23, r24, R25, and R26; B is phenyl substituted with R9, Ri0, Rii, R12, and r13; of which R6, R9, R1 丨, R 丨3. R22, R23, R25, R26, R27 and R28 are hydrogen; R24

I Compound No. r3 / r4 R9 R10 R12 R24 856 h / cf3 H Cl Cl Nando-2-oxy 857 h / cf3 Cl HH p dense lake 2-oxy compound of formula I, where A is C and forms hexahydro Pyridine ring; m, p, q, and r are 0; s is 1; η is 0; a double bond is formed between the methyl carbon (a) and the 4-position of the hexahydropyridine ring; R8 is R22, r24, R25 and R26 substituted pyridin-3-yl; E series- (CR27R28) X- (CR29R30) factory (where \ series 1 and y series 〇); B series substituted with R9, R10, Rn, R12 and ruler 3 Phenyl; of which R2, R3, R5, R6, R9, R10, R12, R13, R22, R25, R26, R27 and R2s are hydrogen; 90038 -155- 200427680

Compound number _ 'Rn__ 858 CF3 CF3 phenoxy 859 __CF3_ oxidin-2-ylamino group of formula I compound, in which the eight-series CH forms a hexahydropyridine ring; n-series 1, from methyl carbon (a) and its Substituents form single bonds; ρ is 0; q and r are 1, forming N-substituted oxy derivatives; m and s are 1; B is a bridging group from methyl carbon to R; where R is R17, R18, R19, R2. And R21 substituted phenyl; E is-(CR27R28) x- (CR29R30) y- (where X is 1 and y is 0); and R8 is phenyl substituted with R22, R23, R24, R25 and R26; Ri, R2, R3, R6, R2i, R22, R23, R25, R26, R27 and R28 series hydrogen:

90038 -156- 200427680 Compound number _B_R15 R4__j ^ 7 r19 r24 _-Qg (= 〇) NR15 H Cl pyridine-2-oxy compound of formula I, in which A is CH and forms a hexahydro p ratio ring; i, forming a single bond from methyl carbon (a) and its substituents; ρ is 0; m and s are 1; B is a bridging group from methyl carbon to R; wherein R is R17, R19, r20, and R21 substituted phenyl; q is 0 and! · System 1, forming oxides; e- (CR27R28) x- (CR29R30) plants (where X is 1 and y are 0); and R8 is phenyl substituted with R22, r23, r24, r25, and R26; of which Rl, R2, R6, R21, R22, R23, R25, R26, R27 and R28 series hydrogen:

Compound No.B R4 R17 / R18 Rl9 / R20 R24 861 0C (= 0) NR15 * CF3 H / FH / F 6-chloropyridine-3-oxy862 0C (= 0) NR15 CF3 H / H Cl / H CH = N0C2H5 863 0C (= 0) NR15 Cl H / H OCF3 / H pyridin-2-oxy * R15 hydrogen in compound 861-863. 1 gaseous salt; 2 trifluoroacetate; 3 succinate; 4 tartrate; 5 bromide salt; 6 oxalate; 7 chloride salt, monohydrate; 8 ethanesulfonate; 9 ethyl 90038- 157-200427680 based sulfate. The following table sets forth the physical characterization data of the compound of formula I of the present invention: Table 2 Physical characteristic compound number Experimental formula Physical state / Solubility point (° C) 90038 1 c18h19n — 2 c18h19n.hci — 3 C18H19N.HBr solid, 200 4 C18H18C1N_HC1 — 5 c18h18cin.hci — 6 c18h18cin.hci — 7 c18h17f2n.c2h2o4.h2o — 8 C2〇H17F3N6 solid, 93-95 9 c2〇h17f6no2 oil 10 C22H27N oil 11 C19H20C1N.HC1 — 12 C21H19F2N28F3N2O , 105-107 15 c28h25f2n30s solids, 228-230 16 c27h26fn30s solids, 153-155 17 c27h25f2n3os solids, 134-137 18 c28h32f6n2.hci — 19 C30H34N2.HC1.H20 — 20 C22H28N2 liquid 21 C30H30N2 105 107 22 C25H30N2O2-23 c25h31n202s2 solids, 136-137 24 Ci8H18C1N.HC1-25 C30H33N3O -158- solids, 159-160 200427680 compound number conventional physical state / melting point (° c) 26 C31H35N3O solids, 134-135 27 c22h22n2s — 28 c25h23cifn oil 29 c25h23f2n oil 30 c26h24f3n oil 31 c26h23f4n oil 32 c26h24f3n〇 oil 33 C27H22BrF6N solid 34 C 26H23F4N viscous oil 35 C26H23F4NO oil 36 c25h22cif2n viscous oil 37 C25H22F3N viscous oil 38 c26h22f5n viscous oil 39 c26h26cin〇 viscous oil 40 c26h26fno solid, 87-89 41 c27h26f3no viscous oil 42 c35h25f -89 44 C28H31N03 solid, 114-115 45 c3〇h29f6no solid 46 c29h27f6no solid 47 c30h29f6n〇3 solid 48 c3〇h29f6no3 oil 49 c31h31f6n〇4 oil 50 C30H27F6NO2 viscous solid 51 C3iH29F6N20 viscous 53C20 The solid 54 C29H26F6N202 200 427 680 55 90038 C30H28F6N2O2 -159- solid Empirical formula C31H30F6N2O2 C31H30F6N2O2 C32H32F6N202 C3iH3〇F6N202 c3〇h28f6n2o C3iH26F6N2OS C32H26F6N2C) C32H25C1F6N2〇c32h25cif6n203 c32h25cif6n2o c32h25cif6n2o c33h25f9n2o C33H25F9N203 C33H25F9N20 c33h25f6n3〇c33h25f6n3o C32H25F6N303 C34H29F6N303 C28H25C1F3N5 c29h25f6n5 c28h28cin5 c28h27ci2n5 c28h27f2n5 c28h27cifn5 C29H28F3N5 c29h27f4n5 c3〇h27f6n5 c30h25f4n5 〇4 c26h25cin2s c27h28no Compound No. 56 57 58 59 60 61 62 63 64 65 66 67 68 69 70 71 72 73 74 75 76 77 78 79 80 81 82 83 84 85 Physical state / Melting point (° c) Sticky solid solid, 60-65 solid sticky solid solid solid solid solid solid Solid solid solid solid oil solid, 58-63 solid oil oil solid oil oil solid, 104-106 solid 90038 -160- 200427680 experimental formula C27H22BrF6N〇C27H21BrF7NO C25H22CIF2NO C25H22F3N〇2 c26h22f5NO2 C27H26C1N〇2 c26h26fno2C27F2 c27h2 4 C3iH29F6N02 c30h27f6n〇3 c31h29f6no3 c3〇h28f6n2〇3 C31H30F6N2O3 C3iH3〇F6N2〇3 c32h32f6n203 C3iH26F6N202S c32h26f6n202 c32h25cif6n202 c32h25cif6n2〇2 C33H25F9N202 C33H25F9N2〇2 C33H25f6n3o2 c29h25f6n5〇c28h27ci2n5〇c3〇h27f6n5o C3〇H25F4N5〇5 -161-- compound No. 86 87 88 89 90 91 92 93 94 95 96 97 98 99 100 101 102 103 104 105 106 107 108 109 110 111 112 113 114 115 900 38 Physical state / melting point (° c) solid solid solid, 90-96 solid, 159-160 solid, 162 -167 solid, 155-163 solid 179-183 solid, 158-162 sticky solid solid solid, 76-80 sticky solid solid solid solid solid solid solid sticky solid solid solid solid solid solid solid, 90-95 sticky solid solid 200427680 compound numbering experiment Formula Physical state / Melting point (° c) 116 C40H43F4NO4.HBr solid, 121-123 117 c35h30f6n2o solid 118 C4〇H38F6N2〇4.HBr solid 181 C34H30F5N3O5 solid, 98-103 182 c30h31cif3n3o3 solid foam 183 C30H29Bi Oil 185 C30H3iF4N3〇4 Oil 186 C29H29F4N304 Oil 187 C30H31F4N3O4 Oil 188 C3〇H3〇C12F3N3〇3-189 c30h3Gci2f3n3o3 — 190 C3〇H3〇C12F3N3〇3 — 191 c30h30ci2F3N3F3N3〇3 — 191 c30h30ci2F3N3O3 Sticky solids 195 C30H30F5N3O4 Oil 196 C30H30F5N3O4 — 197 C32H34F5N303 — 198 C30H30F5N3O3 — 199 C30H30F5N3O3 — 200 C30H30F5N3O3 — 201 C30H29F6N3O3 — 202 C30H3F3N3F6N3203 206 C3iH30C1F6N3O3 — 207 90038 C3iH3〇C1F6N3〇3 -162- 200427680 Compound number conventional physical state / melting point (° c) 208 C3iH3〇BrF6N3〇3 — 209 c3 丨 h34f3n3〇4 — 210 C32H35C1F3n3f3n3f- 〇3 --213 c36h36f3n3〇3 - 214 C34H34F3N303 - 227 C32H29C1F3N3〇3 --228 c32h28ci2f3n3〇3 - 229 c32h28ci2f3n303 - 230 c32h28ci2f3n3〇3 - 231 c32h28ci2f3n303 - 232 c32h28ci2f3n3〇3 - 233 c32h28ci2f3n3o3 - 234 c32h27ci2f3n3〇3 - 235 c32h29f4n304 Solid, 73-78 236 C32H29F4N304 solid, 75-80 237 C32H28F5N303 — 238 C32H28F5N304 solid, 65-70 239 c32h28f5n3〇3 — 240 C32H28F5N303 — 241 C32H28F3N33 — 245 f3N33 — 245 cf Solid, 75-80 247 c33H28cif6n3〇3 — 248 C34H28F9N303 — 249 90038 c33h29f6n3o4 -163- 200427680 Compound number Experimental formula Physical state / Melting point (° c) 250 c38h34f3n3〇3 — 251 C38H34F3N303 261 c30h31f3n6o3 solid foam, 70-75 262 c29h28cif3n6〇3 solid foam, 65-69 263 c29h28cif3n6〇3 solid foam, 79-83 264 c28h28ci2n6o2 solid 265 c3〇H3〇cif3n6o2 — 267 c29h3 8f 3f 〇H3〇cif3n6〇3 solid foam, 85-89 268 C3〇H3〇BrF3N602 — 269 C3〇H3〇BrF3N6〇2-270 C3〇H3〇BrF3N6 03 solid foam, 93-97 271 C30H30F3IN6O3 solid foam, 89- 92 272 C29H28F4N6O3 solid foam, 66-70 273 C29H28F4N6O3 solid foam, 80-84 274 C28H28C1FN6〇2 solid 275 C29H28F4N603 solid foam, 78-81 276 c29h29f4n6o3 277 C30O3F3C3H3F3N2 2 — 281 c3〇h29ci2f3n6o2 — 282 c3〇h29ci2f3n6o2 — 283 c30h29ci2f3n6〇2 — 284 c3〇h29ci2f3n6o2 — 285 c31h33f3n603 solid foam, 81-83 286 c33h37f3n6o3o3 foam, solid state C3iH30F6N6O2 -164- 200427680 Compound number Experimental formula Physical state State / mp (° c) 289 c3, h3〇f6n6o2 solid foam solid c30h28f6n6〇3 290, 70-80 291 C3iH30F6N6O3 gum 292 C3iH29C1F6N602 - 293 C32H29F9N602 - 294 C30H28F6N6O4 Solid, 70-80 295 C31H30F6N6O4 296 C3〇H3〇F3N7〇 gum 5 — 297 c36h35f3n6o2 — 298 c36h35f3n6〇3 — 302 c31h3〇f6n6o2s semi-solid 304 c31h31f6n5o2 gel 305 c31h31f6n5o3 gel 306 c31h32f3n9o2 solid 148-155 307 c31h29c3f3f6n6f6n6f6n c29H3〇cif3n6o slurry 312 C29H3〇BrF3N (50 semi-solid, 56-61 313 C29H30F4N6O slurry 314 C29H30F4N6O slurry 315 C29H30F4N6O slurry 316 c29h3 slurry 3C3N3O3C30H3f3c6H30f Semi-solid, 57-62 321 C29H29F3N602 solid, 180-184 322 90038 c29h28cif3n6o2 -165- solid, 173-175 200427680 Compound No. 323 324 325 326 327 328 329 330 331 332 333 334 335 336 337 338 338 339 340 341 342 343 344 345 345 346 347 3 4,834,935,035,135,290,038 c29h28cif3n6〇2 c29h28cif3n6〇2 C29H28BrF3N6〇2 empirical formula C29H28F4N6O2 C29H28F4N6O2 C29H28F4N6O2 c29h28f3in6o2 C30H3iF3N6〇2 c30h3 Shu f3n6〇3 C30H28F6N6O3 C29H28F3N704 C29H29C1F3N702 c29h29cif3n7〇2 C29H29C1F3N702 C29H29BrF3N7〇2 c29h29f3in7〇2 C29H29F4N7O2 C29H29F4N7O2 C29H29F4N7O2 C30H29F6N7O2 C30H32F3N7O2 c30h32f3n7〇3 C30H29F6N7O3 C29H29F3N804 c29h28cif3n6〇3 c29h28cif3n6〇3 c29h28cif3n6〇3 C29H28BrF3N6〇3 C29H28F4N6O3 C29H28F4N6O3 -166 - physical state / mp (° c) a solid, solid 143-146, 217-220 solid, solid 217-220, 141-144 solid, 151 -159 solid, 195-198 solid, 225-229 solid, 215-218 solid, 204-209 solid, 210-213 solid, 232-236 solid foam, 86-90 solid foam, 75-78 solid foam, 89-93 Solid foam, 94-99 solid foam, 84-88 solid foam, 89-92 solid foam, 74-78 solid foam, 142-149 solid foam, 198-200 solid foam, 83-87 solid foam, 93-98 solid foam , 83-88 solid foam, 105-110 solid foam, 76-79 solid Solid foam, 58-61 solid foam, 153-156 solid foam, 73-76 solid foam, 76-80 solid foam, 63-69 200427680 compound number conventional physical state / melting point fc) 353 C29H28F4N6O3 solid foam, 92-95 354 c29h28f3in6〇3 solid foam, 73-75 355 c30h31f3n6〇3 solid foam, 73-76 356 c30h31f3n6〇4 solid foam, 73-75 357 C3〇H28F6N (5 04 solid foam, 69-72 358 C29H28F3N705 solid, 143- 146 395 c32h29cif3n3〇4 — 396 c32h28ci2f3n3〇4 — 397 C32H28F5N304 — 398 C33H29F6N304 — 399 c29h28cif3n6 04 solid 400 C29H28F4N604 solid 401 C30H30F4N6O4 solid, 130-137. 3〇 ^ 28 卩 6 wind 〇4 solid, 138-142 403 C3iH3〇F6N6〇5 solid foam, 118-122 404 c30h28f6n6〇5 solid, 136-140 405 C3iH3〇F6N605 solid foam, 120-125 427 C29H32F3N303 oil 429 C29H32F3N303 Oil 432 C32H36F3N303 Oil 433 c25h31f3n603s Oil 434 c28H26f6n6o2 Oil 435 C27H26C1F3N60 Liquid 436 c31h29f3n403 White solid 437 C3iH27F6N302 Paste 438 C3iH27F3N4O4 316 c3h3f3n4o4 90038 Compound No.Experimental Physical State / Melting Point (° c) 443 C30H27C1F3N3〇2 Sticky solid 444 c31h29f3n4〇3 White solid 445 c31h28cif3n4〇3 White solid 446 C32H28F3N503 Solid 447 C31H28C1F3N4〇3 White solid 448 C32H28F6N3N4 Solid 3450 3 White solid 451 c31h27ci2f3n4o3 — 452 c29h26cif3n4o2 Sticky solid 453 c26h25cif3n7o2 Solid 454 C30H30F6N2O2 Sticky solid 455 C32H28F6N202 Sticky solid 456 c31h27f6n3O3 Solid 457 C35H42F3N305 459 C27H25ClF4N2〇3 solid solid solid 458 C27H26F4N203 460 461 c27h24f6n2〇3 c27h24cif5n2〇3 solid solid solid 462 C27H24F5IN203 c27h26cif3n2〇3 solid 464 C27H25F5N203 463 465 C27H27C1F3N302 solid solid solid 466 C27H26F5N302 467 468 C28H28F4N204 c32h35f5n2〇2 solid solid solid 469 C28H27F5N204 470 C29H32C12N203 — 471 C29H32C1FN2〇3 — 474 c30h32cif3n2〇3 -168-200427680 Compound No. Experimental formula Physical state / melting point (° c) 473 C30H32C1F3N2〇3 — 474 c29h31cif22 —3 — 475 c29h32cifn2 — 2F3 — 3 478 c30h32f4n2〇3 --479 c29h31f3n2〇3 --480 C29H3iC13N2〇3 --481 c29h31ci2fn2〇3 - 482 C29H30C12F2N2O3 - 483 C30H31Cl2F3N2O3 - 484 c30h31ci2f3n2o3 - 485 c30h32cif3n2o3 - 486 c30h32f4n2〇3 - 487 c30h31f5n2o3 - 488 c31h32f6n2o3 - 489 C3iH32F6N2〇3 --490 c30h32cif3n2o3 solid 491 C30H3iF5N2 0 solid 492 c31h32cif3n2 04 solid 493 C3iH31F5N2 04 solid Body 494 c29h29cif3n3〇3 solid 495 C29H28F5N303 solid 496 C3iH32F5N3〇3 solid 497 C32H34F5N303 solid 498 C29H28F5N304 solid 499 C30H30F5N3O4 solid 500 C30H33C12N3O4 — 501 C30H3C3C3C3O3C2C3O3C2C3O3C2O --504 c30h33f2n3〇4 - 505 c30h32f3n3o4 - 506 c30h32ci3n3o4 - 507 c30h31ci2f2n3o4 - 508 C30H32C13N3O4 - 509 C30H32Cl2FN3O4 - 510 c3〇h31ci2f2N3〇4 - 511 C3iH25F6N30 512 c31h32f5n3o4 solid solid 513 C31H33C1F3N305 - 514 C31H33F4N305 - 515 C31H32F5N305 - 516 C34H31F5N404 solid, 95-110 517 C30H31F5N4O3 solid 518 C30H31F5N4O2S 519 C30H31F5N4O3 solid 520 C32H36F5N406P solid solid solid 521 C29H30F5N3O4 solid 522 c31h31f5n4o5 c29h31ci2n3〇3 523 - 524 c29h31cifn3o3 - 525 c29h30cif2n3〇3 - 526 C29H31C1FN303 - 527 C29H31F2N303 - 528 C29H30F3N3O3 - 529 C29H30C13N3O3 - 530 C29H30C12FN3O3 - 531 C29H29C12F2N3 03 — 532 90038 C29H3GC13N303 -170- 200427680 Compound No. Experimental formula Physical state / Melting point (° c) 533 C29H3〇C12FN3〇3 — 534 C29H29a2F2N3〇3 — 535 C30H31F4N3O3 solid, 63-73 536 C31H34F3N303 C1F3C3O3H3C3O3 - 539 C31H29C1F3N303 C3iH28F5N3〇3 solid solid 540 541 C31H34F5N304S - 542 C32H34F5N304S - 543 C33H30C1F3N2O2 solid solid 544 C33H29F5N202 545 546 C33H29F5N203 C33H3〇C1F3N2〇3 solid solid solid 547 C33H28F6N203, 58-67 548 C33H27F7N203 solid, 72-81 549 c34h31f5n2o3 solid 550 c34h29cif5n3o3 552 C34H28F7N303 551 c34h28ci2f5n303 solid solid solid solid 553 c35h32f5n3o4 554 C35H32F5N304 555 C30H2SF4N4O2 solid solid solid 556 C30H27F5N4O2 557 558 C29H26F5N502 c29h27f4n5〇2 solid solid 559 solid 560 c29h25f5n4o2s c29h26f4n4〇2s 561 c29h25ci2f3n4o3s solid solid 562 90038 C29H24C1F5N403S -171 - solid experiment compound No. 20042768090038 Physical state / melting point ct) 563 c30h29f5n4〇3 Body 564 c29h31cin6o2 - 565 c30h31f3n6o2 - 566 C30H30F4N6O2 - 567 C29H30C12N6〇2 - 568 c29h29ci3n6o2 - 569 C29H29ClF2N6〇2 - 570 c29h29cif2n6o2 - 571 C3〇H3〇C1F3N602 - 572 c29h29ci3n6o2 - 573 c29h28ci4n6o2 - 574 c29h28ci2f2n6o2 - 575 c29h28ci2f2n6o2 - 576 c30h29ci2f3n6o2 - 577 c29h29ci3n6o2 - 578 c29h28ci4n6〇2 - 579 C29H28C12F2N602 - 580 C29H28C12F2N602 - 581 c3〇h29ci2f3n6o2 - 582 c29h3Gcifn6o2 - 583 c29h29ci2fn6〇2 - 584 C29H29F3N602 - 585 C29H29F3N602 - 586 C3〇H3〇F4N (5〇2 - 587 C30H30F4N6O2 - 588 C29H29C1F2N602 — 589 C29H28F4N602 — 590 c29h29cif2n6o2 — 591 C29H28C12F2N602 — 592 C29H28F4N02 -172-200427680 90038 Compound Number Physical State / Melting Point (° c) 593 C29H28F4N6O2 — 594 c3oh29f5N2O6O2 — 598 C30H32F2N6O2 — 599 C3iH33F3N6〇2 — 600 c31h33f3n6o2 — 601 c30h33cin6〇3 — 602 c30h32ci2n6〇3 — 603 C3〇H32F2N6〇3 — 604 C30H32F2N6O3 — 605 c31h33f3n6o3 — 606 c31h33f3n6〇3 — 607 c36h38n6o3 — 608 c31h35cin6o4 — 609 c31h34f2n6〇4 — 610 C30H2C35H2F5 614 C35H34F2H502 — 615 C36H35F3N602 — 616 c35h35cin6〇3 — 617 c35h34ci2n6〇3 — 618 c35h34f2n603 — 619 C35H34F2N603-620 C36H35F3N603 — 621 C41H40N6O3 — 622 C33H6N # 2C3H40N6O-C3H6N 2 - 624 c33h32ci2n602 - 625 c33h32f2n6o2 - 626 c33h32f2n6〇2 --627 c32h29cif3n3〇2 solid solid 628 C32H28F5N302 629 C3iH29C12N3〇3 --630 C3iH29C1FN3〇3 --631 c31h28cif2n3〇3 - 632 C33H34C1N303 - 633 C33H34C1N305 - 634 C32H29C1F3N3〇3 - 635 c32h29cif3n3 〇3 — 636 C33H31C1F3N303 White solid 637 C34H33C1F3N303 White solid 638 C33H32C1N305 — 639 c31h29cifn3〇3 — 640 c31h29f2n3〇3 — 641 c31h28f3n3o3 — 64 2 C32H29F4N303 - 643 c32h29f4n3〇3 --644 c31h29ci2n3〇5s --645 C3iH28C13N3〇3 - 646 c31h28ci2fn3o3 - 647 c31h27ci2f2n3o3 - 648 c32h31ci2n3〇4 --649 c33h33ci2n3〇5 --650 c32h28ci2f3n3〇3 - 651 c32h28ci2f3n303 - 652 90038 C32H29C1F3N303 -174- 200427680 compound No.Experimental Physical State / Melting Point (° C) 653 c32h29f4n3〇3 — 654 c32h2Sf5n3〇3 — 655 c33h29f6n3o3 — 656 c33h29f6n3〇3 — 657 C32H30F3N3O3 — 658 C33H32F3N303 white solid C65H32F3N3O3F3N3 663 c33h31cif3n3o3 tan solid oil 664 c32h29cif3n3o3 665 c32h29cif3n3o3 yellow solid solid 666 C32H29C1F3N303.HC1 - 667 c32h29cif3n3o2s - 668 C32H29C1F3N305S - 669 C32H29C1F3N304 solid white solid 671 670 c33h28cif3n4〇3 c33h28cif3n4〇3 white solid viscous oil 673 672 C32H29BrF3N3〇3 C32H29BlF3N3〇3 Tan solid 674 C32H29F4N3O3 yellow paste 675 C32H29F4N3O3 — 676 c33h31f4n3 3 oil 677 C32H29F3IN303 solid, 85-99 678 C33H3 () C12F3N303 oil 679 c32h28f5n3o3 solid 680 C32H28F5N303 solid 681 C32H28F5N302S — 682 90038 c32h28f5n3〇4 -175-white solid 200427680 compound C ° H3C3 ° C3 ° C27 3 solid, 81-91 684 c32h27cif5n3 solid, 61-77 685 C32H27C1F5N303 solid, 76-83 686 c32h26ci2f5n3 solid, 78-90 687 C33H27F5N4〇3 white solid 688 c33h27f5n4 03 white solid 689 c33h27f -86 690 C33H27F8N303 solid, 77-86 691 C33H27F8N303 solid, 80-88692 c33h29f6n3〇2s - 693 c33h29f6n302s - 694 C34H34F3N303 695 C34H34F3N303 oil oil 696 C33H32F3N305S - 697 C32H27F6N303 698 C34H34F3N304 oil as a white solid solid 700 C33H31F4N304 699 C33H31C1F3N304 solid 701 C33H30F5N3O4 - 702 C33H32F3N303S — 703 c33h29f6n3〇3s — 704 C33H29F3N403 — 705 C34H32F3N304 — 706 c32h29cif3n3 05 solid 707 C33H28C1F3N404 white solid • 708 c33h28cif3n4 04 white solid 70 9 c32h28f5n3o5 solid 710 C33H27F5N404 white solid 711 c33h27f5n404 white solid / 712 90038 C3〇H28C12N4〇3 -176- 200427680 compound number conventional physical state / melting point 〇 :) 713 C3〇H28C1FN4 〇3 — 714 c3〇h27cif2n4〇 C3〇H28C1FN4〇3 — 716 C30H28F2N4O3 — 717 C3〇H27F3N4〇3 — 718 c30h27ci3n4o3 — 719 C3〇H27C12FN4 03 — 720 c3〇h26ci2f2n4 3 — 721 c30h27ci3n4O3 solid 3f2 solid 3722 724 c31h27ci2f3n403 solids 725 c31h27ci2f3n4〇3 solids 726 c30h27ci3n4〇3 — 727 c3〇h27ci2fn4〇3 — 728 c3oh26ci2f2n4〇3 — 729 c31h28cif3n4o3 solids, 94-104 732c3H27f31h3f27n31 c31h28cif3n4〇4 — 734 C31H28F4N404 — 735 C31H27F5N404 — 736 C3iH27F5N4〇3 solid 737 c31h27ci2f3n4〇3 solid 738 c31h26cif5n4o3 solid 739 c3〇h26f5n5〇3 740 C3H30F3N30F Body, 136-142 200427680 compound number 743 744 745 746 747 748 749 750 751 752 753 754 755 756 757 758 759 760 761 762 763 764 764 765 766 767 768 769 770 771 772 90038 experimental formula C30H30F5N3O4 C3iH28F5N3c3c3c3c3c3c3 5 C33H3〇C1F3N2〇3 C33H29F5N203 c33h29f5n2〇4 C33H28F6N204 c33h27f7n2〇4 c31h28f3n3o4 C32H28F5N304 C32H28F5N3〇4 c32h27cif5n3〇4 C32H27C1F5N304 C32H27C1F5N3〇4 c32h26ci2f5n3〇4 c33h27f8n3〇4 C33H27F8N304 C34H31F5N405 C31H28ClF3N4〇4 c31h27f5n404 C3lH27F5N4〇4 C31H27F5N404 C3iH27F6N3〇4 c31h27ci2f3n4〇4 c31h26cif5n4〇 4 C28H29F3N202 C29H31F3N204 C27H28F3N303 c27h28f3n3〇2s -178-physical state / melting point (° c) solid, 138-143 solid solid solid solid solid solid, 135-144 solid, 14M46 solid solid solid, 145-148 solid, 157-161 solid , 137-142 solid, 172-174 solid, 142-144 solid, 159-161 solid, 149-153 solid, 17M75 solid solid solid, 150-153 solid solid, 152-154 solid, 15M54 solid gum white solid yellow solid 200427680 Compound Number Permanent Physical State / Melting Point (° c) 773 c26h32f3n303 solid 774 c28h3Qf3n3o3 tan solid 775 c29h32f3n3o3 oil 776 C29H32F3N303 oily solid 777 C29H32F3N302S yellow solid 779 C30H34F3N3O3 yellow solid 779f30C3 303 f3n3O3 solid 779f30c3 782 c32h36f3n3o3 oil 783 c30h32f3n3o5 solid oil 785 C29H32F3N304 784 C32H36F3N305 786 c31h25f5n403 solid solid solid c31h25f5n4〇4 85-92787, 137-141 788 C29H25F6N02 789 C27H26C12N202 solid solid solid 790 C29H26F6N202 791 C29H26F6N204 792 C31H30F6N2O2 solid 793 C29H32N202 solid solid solid 794 C29H30F2N2O2 795 c29h28ci4n2o2 c29h28ci4f2n2〇2 solid solid 796 solid 797 C31H28F6N202 798 799 C32H30F6N2O2 solid 800 c30h3〇ci2n2o2 c30h30ci2n2〇2 solid solid solid 801 C29H26C12N202 200 427 680 802 90038 C3iH26F6N202 -179- solid empirical formula c28h25f6no3s C30H29F6NO3S C28H26F6N202S c33h26f7no c32h26f6n2 c3〇h28n2o c3〇h26ci2n2o c3〇h26f2n2o C 32H27F6N3 c29h25ci2n3〇c29h23ci4n3o c30h25cif3n3〇c30h25cif3n3〇c30h25cif3n3o c30h25f4n3〇c3〇h24ci2f3n3〇c30h24ci2f3n3o C30H24F5N3O c3〇h24cif4n3〇c31h25f6n3o C3iH29F6N30 C3iH25F6N3〇C3iH25F6N30 c31h24cif6n3o C27H26Cl2N2〇3 C29H26F0N203 C29H26F6N205 C3iH3〇F6N2〇3 c29h3〇ci2n2〇3 C29H30F2N2O3 -180- Compound No. 803804 805 806 807 808 809 810 811 812 813 814 815 816 817 818 819 820 821 822 823 824 825 826 827 828 829 830 830 831 832 90038 Physical state / Melting point (° c) Solid solid solid solid, 50-59 solid solid solid paste Paste solid solid solid solid solid solid solid solid solid solid solid solid solid paste solid solid solid, 68-77 solid solid solid solid solid solid 200427680 compound number experimental formula physical state / melting point (° c) 833 C29H28Cl4N2 03 solid 834 c29h28ci2f2n2〇3 solid 835 c3 丨 h36n2〇5 solid 836 C3iH28F6N2〇3 solid 837 c32h30f6n2〇3 solid 838 C3iH26F6N2 03 solid 839 c33h26f7n〇2 solid, 171-173 840 c32h26 841 c30h26ci2n2o2 f6n2〇 solid solid solid 842 C30H26F2N2O2 843 844 c29h25ci2n3〇2 c32h27f6n3〇 paste c3〇h25cif3N3〇2 solid solid 845 solid 847 846 c30h25cif3n3o2 c30h25cif3n3〇2 848 C30H25F4N3O2 Solid 849 C29H23C14N3〇2 solid solid solid 850 851 c30h24ci2f3n3o2 c30h24ci2f3n3〇2 853 C31H25F6N302 852 c30h24cif4n3〇2 solid solid solid solid 854 C31H25F6N302 855 C31H24C1F6N302 solid 128-135856 c30h24ci2f3n3〇2 c30h25cif3n3〇2 solid solid 857 858 C32H26F6N20 859 c30h25f6n5 solid solid solid 861 860 C34H34C1F3N304 C2H504S C32H27C1F5N3〇4 solid, 158-161 862 c30h31cif3n3o4 Solid 863 C32H29ClF3N3 05. Solids were evaluated for the activity of candidate insecticides against tobacco moths in a surface-treated feed test (Heliothis virescens [Fabricius]). 0090038 -181-200427680 In this test, 1 ml of molten (65-70 ° C) Wheat germ-based artificial feed inhaled 4x6 multi-well flat pan (24 wells) (ID # 430345-15.5mm diameter xl7.6mm depth; Massachusetts Corning Costar, OneAlewifeCenter 02140, Cambridge). Allow feed to cool to ambient temperature before treating with candidate insecticides. In order to determine the insecticidal activity, a candidate insecticide solution for testing using Packard 204DT Multiprobe® Robotic System (Packard Instrument Company of Meriden 800 Research Parkway 06450) was prepared. A 1:50 water / acetone solution (volume / volume) is diluted with a stock solution to water / acetone ratio of 1: 7 to a standard 50 millimolar candidate insecticide in DMSO. 40 microliters of the solution thus prepared was then pipetted onto the feed surface in each of three wells of a 24 multi-well plate. This process was repeated with 7 other candidate insecticide solutions. Once processed, the contents of the multi-well pan are allowed to dry, leaving a 0.25 millimolar candidate insecticide or 0.25 millimolar concentration on the surface of the feed. Appropriate untreated controls containing only DMS0 on the surface of the feed were also included in this test. In order to evaluate the insecticidal activity of candidate insecticides at different application rates, a test was established using the most frequently used standard 50 millimolar candidate insecticide in DMSO as described above. For example, a standard 50 millimolar solution is diluted with DMSO in a mechanical system to obtain a candidate insecticide solution of 5, 0.5, 0.05, 0.005, 0.0005 millimolar or less. In these evaluations, the surface of the feed in 24 multi-well plates was repeated 6 times at each application rate, with a total of 4 candidate insecticide application rates in each plate. 90038 -182-200427680 Put two tobacco moth second-instar larvae into each test well, and each privately about 5 hairs {After putting the larva in each well, put the flat plate with: Ming Sealed with poly film adhesive tape. Perforate the tape on each well to confirm the supply of Shida's i gas. The plate was then fixed in a growth chamber at 25 ° C and 6⑽ relative humidity for 5 days (14 hours / day in sunlight). After the exposure period of each day, the insecticidal activity of each candidate insecticide application rate: Insect activity based on the weight of insects relative to the weight of untreated control insects. Assess percentage of lethality during comparison. In Table 3, insecticidal activity is provided for the application rates selected from this experiment. The test compounds of formula I are identified by the numbers in Table 1 and those in Table 1. Table 3 Insecticidal activity of the test compounds on the surface of the feed of Μ / 于 and tobacco E. 90038 -183- 200427680 涔 冷 赉 田 ^^ 鱼 Illi ^ rrb ▲ b 命 穿 翁 转 阼 &gt; 坌 坌 ai, v tb -X.CV Ling Chuan Weng Binding 涔 Cold 赉 Wang Chuan Weng Xian! -Sl ^^ — 涔 Two 赉 into b life 棼 棼 100 100 100 00 57 33 50 98 30 100 Μ 51 0 26 60 100 100 70 100 100 80 100 100 100 100 1000 50 100 81 71 W &quot; 30 61 Ί ^ Γ 100 52 — ^ 1 00 31 17 99 100 100 100 50 100 100 109 100 100 111 50 100 Two 2 Τ5ί 100 100 100 Two 3 50 100 100 100 Two払 100 100 100 100 two 5 100 100 100 100 liz— Tsl— 100 100 100 100 100 100 100 101 100 100 102 82 s 72 100so 62so 100 53 Ο 100 払 2so 100 7 Ren 100 100 63 33 100 M 755 &quot; 100 67 100 55 5i ° l 50 g so 100 75 3101% 85 1007 T55 &quot; so 103 76 H 91 65 10 ° l 100 56 100 57 100— 100 66 50 50 77 1001 100 93 33— 97 12 58 i ^ l 100 67 Ο 98 78 67 — 100 N1 loo 100 105 68so 100 79 SI 100 N—loo— 100 106 59 Η 59 kernel 5 H 24 kernel 6 510 50 47 H two 10 ° | 100 50 1 ^, 96 90038 -184- 200427680 lethal growth Restrain Control percentage lethal growth inhibition percentage compound number lethal growth inhibition percentage compound number lethal growth inhibition percentage compound number lethal growth inhibition compound number budding cold ε Η such as compound number I 〇 〇〇〇〇〇〇〇〇〇〇〇〇〇〇 〇 〇〇〇 〇〇 〇5 〇 〇〇 〇〇 〇〇 〇〇 〇5 5 〇 〇5 5 〇 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 00 100 100 247 248 249 250 251 261 262 263 264 Μ * — * Η— LO. 〇 〇 〇〇〇〇 Ο ι—Λ LO Ο Ο ν〇〇〇NJ-· —-1 Ο ο ο ο ο (〇 一一 〇 Ο — Ο ο Ν · &⑴; —⑴ ίδ 8- t〇 »— * h—k Ο ο ο ο t〇ι— t—k ο ο each ο ο one by one ο ο ^ ο ο Η— · 1— 厶 ο ο 〇Ν ο ο t〇 »—k μ- * to ο ο νο Ο Ο Κ) ►— · · —» UJ Ο Q ο ο ο ο ο 3 ο ΙΟ Η- Η- LO 〇〇κ &gt; ο ο Κ) ι — Η — * U) ο ο OJ 〇ο t〇! — »(— * Ο ο Public 〇 〇 to — LO Ο Ο Ln 〇 | Ό One one ο ο σ &gt; ο ο NJ one &gt; — LO Ο Ο ο ο 100 100 100 100 100 100 33 100 1〇〇100 100 100 1Ό0 100 100 100 丨 〇〇100 208 209 210 211 212 213 214 227 228 228 S 〇 〇VO Ο Ο to One Q 〇 〇 〇 〇 〇NJ １００ 〇 〇〇 〇S S3 to 一 〇 〇 〇U) 〇 〇to &gt; —4 &gt; — 〇 〇 〇 公 〇 〇t〇η— »&gt; — ο ο ο ο ο ο tsj One by ο ο ο ο ο 3 S ο 1— * 〇〇〇〇〇〇〇 Ο S Ο 〇〇〇 〇 VO 5 〇— 〇 〇h—A Ι ^ Λ Ό ο ο Ο Ο S ο ο ο ο ο ο -&gt; ο ο S ο ο 4 ^ Ο Ο S ο ο ^ ο ο ο ο ΟΝ ο ο &lt; ο ο ο ο οο οο OC κ &gt; οο LP 2 Η— * ο CO On ο οο οο 90038 -185- 200427680 Lethal Growth Percent Growth Inhibition Lethal Growth Percent Growth Inhibition Compound No. Lethal Rate i Growth Inhibition Percent Compound No. --------._------------- 1 Lethal Growth Inhibition Percent Compound No. Lethal Growth Percent Inhibition Compound Number Lethal Growth Percent Growth Inhibition Compound Number — Percent Inhibitory Growth Inhibition Compound Number Compound Number 1¾ Ό 〇 LO ^ \ 〇-LA. \ 〇Lr \ Ό Ο 'OO Ό UJ \ 〇ON OO &lt; oooo vC — 50 100 100 100 100 17 0 67 83 100 100 100 100 100 95 78 98 99 325 326 327 328 329 330 331 332 333 100 100 100 100 100 100 100 100 100 92 92 100 100 100 100 100 100 1〇316 317 318 319 320 321 322 323 324 17 100 100 100 100 100 〖〇〇100 33 93 100 92 100 100 100 95 95 59 307 308 309 310 311 312 313 314 315 1 〇100 100 50 100 100 〇00 100 〇100 100 100 100 94 100 100 〖〇 100 100 100 293 294 295 297 298 302 304 305 306 1 100 100 17 100 100 1〇】 〇〇0 100 1〇〇〇〇7979 100 100 〇〇〇〇〇〇〇〇〇 100 284 285 286 287 288 289 290 291 292 100 100 100 100 100 100 100 100 99 〇〇〇〇〇〇〇〇〇〇〇〇〇 100 100 274 275 276 277 279 280 281 282 283 1 265 266 267 268 269 270 270 271 272 273 -186- 90038 200427680 Lethal growth inhibition percentage Lethal growth inhibition percentage Compound number Lethal Rate growth inhibition percentage compound number difficult to call ¥ CV ^ 1 to wear ±: Weng I3i such as. 今 今i rr wear ± cold_ rr Kf · CV ^ Lifetime Compound No. 8 § 3 〇§8 §3 is' 88 88 8-5; 〇100 100 100 100 33 0 100 17 1〇〇100 100 100 100 100 96 100 100 100 448 450 451 452 453 454 455 456 457 ί 33 100 100 100 丨 00 100 50 100】 〇〇 | 100 100 100 100 100 100 100 100 100 1〇 [1 439 440 441 442 443 444 445 446 447! 100 100 100 100 100 100 1〇〇100 100 1 100 100 100 100 100 1〇00100 〖〇〇100! 427 429 432 433 434 435 436 437 438! 83 17 Γ〇〇100】 00 100 83】 〇〇10υ 100 87 100 100 100 1〇〇100 100 '397 398 399 400 401 402 403 404 405 100 100 100 100 83 100 〖〇〇100 50 1〇〇100 100 100 100 1〇〇〇〇100 100 | 352 353 354 355 356 357 358 395 3% — 100 100 100 100 100 50 83 100 100 100 100 100 100 100 100 100 100 View 343 344 345 346 347 348 349 350 351 | 334 335 336 337 338 339 340 341 342 90038 -187-200427680 Fatal Percentage growth inhibition percentage lethal growth percentage growth inhibition compound number Compound No. Lethal Growth Percent Growth Inhibition Compound No. Lethal Growth Percent Growth Inhibition Compound No. Lethal Growth Percent Growth Inhibition ο ο '〇〇η Ό' ~ ι. 〇 \ '-i \ 〇— OJ Ό ι ~~ * ν〇Ό 100 100 100 100 100 100 100 1〇〇〇〇100 100 100 100 100 100 100 100 1 〇〇j -512 513 514 515 516 517 518 519 520 〇〇100 17 100 100 100 100 100 77 98 100 100 100 100 100 1〇503 504 505 506 507 508 509 510 511 Jiw »-» * Ό Ο Ο ^ Ο Ο Η *-* Η- * ν〇Ο Ο Lf \ Ο Ο ^ 1— I— »ο ο ο ο ο Ο Ο Ο Ο Ο Ο '-j Ο ο Η- * 1—» ο ο ο ο ο 1 — * 1— »νο Ο Ο ν〇ο. LA h—k ο ο ο — ο ο Ly &gt; ι— * &gt; — * Ο ο ο — ο ο L / i ι— ι- Ο Ο ο ι · 〇ο ο 1〇〇1〇〇1〇〇100 100 100 1〇〇1〇 () 100 100 100 100 100 100 100 100 100 0 0 100 100 485 486 487 488 489 490 491 492 493 〇33 17 100 100 100 100 1〇1 () 0 68 100 100 100 100 100 】 〇〇 丨 ⑻ 100 476 477 478 479 480 4B1 482 483 484 0000 83 00 0 17 94 99 100 98 100 65 63 92 77 467 468 469 470 471 472 473 474 475_ | 458 459 460 461 462 463 464 465 466 —

90038 188- 200427680 Percent lethal growth inhibition Percent lethal growth inhibition Compound number Percent lethal growth inhibition Compound number Percent lethal growth inhibition Compound number Percent lethal growth inhibition Compound number Percent lethal growth inhibition Compound number Wear ± 呙 rr Number ο δ 〇 〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇〇 100 100 〖00 100 100 100 100 100 100 100 100 100 100 100 100 100 1〇〇〇〇575 576 577 578 579 580 581 582 583 〇17 17 33 50 33 0 100 100 86 99 97 96 100 100 96 100 100 566 567 568 569 570 57) 572 573 574 La &gt;- 1— * Ο 〇 ^ 荽 〇〇〇0000 L / i 1-k ►— ^ 〇〇νο Ο 〇La — · ON OQ Ο Ο Ο L-Λ ι— * I—k as ο ο »— ο ο la ι— &gt; — »σ \ ο ο ο ο 2 泛 〇ϊ 8 ^ ο ο ο ^ ο ο L / \ &gt; — Public 〇 〇〇〇0 〇 〇1— * 4 ^ Ο Ο Ό Ο Ο I—k ) — »MOO to ο ο La &gt; — * η— ο ο U) ο ο LM — ^ Ο Ο 4 ^ Ο Ο L / 1 &gt; — · &lt; — Οι Ο Ο Ο ο ^ ο ο as ο ο 100 100 100 100 100 1〇〇100 100 100 100 100 100 100 100 100 100 1 ⑻ 丨 〇 〇539 540 541 542 543 544 545 546 547 (_Λ ~ — 〇 〇〇 〇 〇 一-«. WOO 〇〇〇La ^ -― 100 〇ro ο 〇 一一 OJ 〇QU) 〇〇La ι ~ ι- OJ ο ο Ο Ο Ο L / i) —k ο ο ο ο α 1 ο ο ΟΝ ο ο 1—4 Q ο. Ο ο ο ο ο ο ο 1 521 522 523 524 525 526 527 528 529 90038- 189-200427680 Percent lethal growth inhibition ft ^ Weng I3i -¾ rr vr Ong rr ^ Percent lethal growth inhibition Compound No. i CV plus Yin Bo Chuan is _ TT Percent lethal growth inhibition Compound No. Compound No. 〇〇〇〇 〇〇 〇〇 〇〇 〇〇 〇〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 00 100 100 50 50 100 100 1 100 100 100 100 100 100 100 100 100 100 638 639 640 641 642 643 644 645 646 Ον g public 〇〇 \ 4 ^ 〇〇 \ &gt; — * | ~ · OJ Q 〇Κ &gt; 〇 U) ο ο WOO Q \) «· J ^ fc u &gt; oo Ren oo 〇S * — * 1 ~» L〇〇 O ^ oo G \ 1— * H- * oo ON oo &gt; — * i— · Lk &gt; oo -joo 83 0 83 16 17 100 0 100 卩 100 48 100 99 72 100 14 100 100 620 621 622 623 624 625 626 627 628 ON &gt; — »— — 〇Q — 〇 Ο σ \ π—. Η — · — Ο ο to ο ο Ον ι— »η- &gt;-* Ο Ο LO Ο Ο Ον — one S 88 〇 \ &gt; — * · — * θ ο ο ^ ο ο — ο σ σ ο ο ο 5 8 S ΟΝ — — Ο ο ν〇ο ο 1〇〇1〇〇100 100 100 100 1〇〇〇〇〇100 1〇〇100 1〇〇100 100 100 100 1〇100 '602 603 604 605 606 607 608 609 610 1〇〇〇〇〇〇〇〇 100 100 100 〇〇〇〇〇〇〇 〇〇100 100 100 100 100 〖〇〇】 〇〇100 丨 00 593 594 595 596 597 598 599 600 601 | 584 585 586 587 588 589 590 591 592 90038 -190- 200427680 Percent lethal growth inhibition Percent lethal growth inhibition Compound number Lethal growth inhibition percentage Compound number Lethal growth inhibition percentage Compound number Fate HJi jrr — lethal growth inhibition percentage compound number rr compound number 〇 〇 〇 〇〇 〇〇 〇〇 〇〇 〇〇 〇〇 〇〇 〇〇 〇〇 〇〇 〇 〇 δ ο ο ο ο ο ο 100 100 50 100 0 100 100 1〇〇〇〇〇100 100 100 100 32 100 100 100 1〇〇! 701 702 703 704 705 706 707 708 709 100 100 100 17 100 100 100 丨 00 100 100 100 100 98 100 100 100 100 100 692 693 694 695 696 697 698 699 700 1〇〇100 100 100 100 100 17 100 100 100 100〇100 100 100 100 100 00 100 100 683 684 685 686 687 688 689 690 691 〇100 100 0 100 100 100 100 100 100 100 100 25 100 100 100 〇〇〇〇〇674 675 676 677 678 679 680 681 682 100 100 0 50 0 〇100 50 100 100 100 100 100 98 91 100 1〇100 665 666 667 668 669 670 671 672 673 ON One one ο ο Ον Ο Ο 〇 \ — One ^ Ο Ο Ο Ο Committee is 0 \) — * &gt; — * α ο ο Ό Ο Ο Ον one one σ \ Ο Ο Ο Ο Ο CJn —-* * 1 σ \ ο ο a ο ο a-α \ ο ο ο ο 〇ν · — * Ον Ο Ο Ο ο 〇 \ — Ον Ο Ο Ο Ο 1 64 7 648 648 650 651 652 653 654 655 191-90038 200427680 90038 -192- 200427680 lethal growth inhibition percentage lethal growth inhibition percentage compound number lethal growth inhibition percentage compound number lethal growth inhibition percentage compound number cv wood α &gt; 1 涔Chuan Ailin · Miscellaneous rr CV 'M rr Lethal Growth Percent Growth Inhibition Compound No. Compound No. OO 〇 〇〇 〇〇 〇〇 〇〇 〇〇 〇 0 00' ο ο ο ο ο ο ο 〇 〇〇 ^ ο ◦ ο ο ο ο 1 8¾ § OO Η- »&gt; —i W 〇 〇〇〇〇〇〇〇〇〇- &gt; 〇 〇— 〇 〇g §3 OO —— woo 〇〇oc — 〇〇CO — v—. OJ oooo OO —— 'UJ ooooo OO-1 ~ 1 — 〇 〇VO 〇 〇〇0 1—i 1—1 NJ 〇〇〇 〇 〇OO 1—1— * ΙΟ ο ο ο ο οο — — (Ο Q 〇Μ ο ο οο &gt; — * »Μ ο ο OJ ο ο ΟΟ ι— * ι ~~ k to 〇〇Α ο ο οο one by one to 〇〇Μ ο ο ΟΟ ι— &gt; -1 Μ ο ο ΟΝ ο ο 〇〇 一一 to ο ο ο ο 100 100 100 100 33 0 100 0 1 〇1〇〇100 100 100 100 100 100 64 100 810 811 812 813 814 815 816 817 818 00 1 — 2 S8 〇〇 ^ S 5 ^ ° S §S i 00 &gt; — * ha S S8 〇〇—— § ο ο 1 governance. 1 So _ So 〇1〇〇100 100 100 33 100 100 1〇70 70 100 100 100 100 87 100 丨 ⑻ 丨 00 792 793 794 794 795 796 797 798 799 800 〇33 100 67 0 100 〇1〇〇100 98 1 〇〇100 100 100 100 98 100 1〇〇783 784 785 786 787 788 789 790 791 — | 774 775 776 777 778 779 780 781 782 193-

90038 200427680 Percent lethal growth inhibition Percent lethal growth inhibition Compound No. CV such as rr Compound No. 100 50 83 17 0 100 100 00 100 0 100 100 100 9-9 46 100 100 100 00 100 83 100 100 50 100 ] 〇〇] 〇〇〇〇〇〇〇〇〇〇〇〇〇〇 100 100 100 〇〇〇〇〇〇〇85 85 856 857 858 859 860 861 862 100 100 100 100 100 100 100 100 83 100 100 100 100 100 100 100】 〇〇 丨 00 846 847 848 849 850 851 852 853 854 | 837 838 839 840 841 842 843 844 845 90038 -194- 200427680 0, 2 5 ml of candidate insecticide on the feed surface These tests. As described in Table 3 above, most of the compounds provided a 100% lethality and 100% growth inhibition of the tobacco moth. Although the invention has been illustrated with preferred embodiments, of course, those who are generally familiar with the art can make use of various preferred variations of the examples, and hope that it can be applied to the invention in addition to what is specifically described herein. . Therefore, the combination of the scope of the invention and the definition of the scope of the present invention is one pound, and there are modifications within the spirit and scope as shown in the following application. `` A Calling Special 90038 -195-

Claims (1)

200427680 Scope of patent application: 1 · A compound of formula I Wherein: m, n, q, and rAS are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is selected from C and CH, forming a group selected from hexahydropyridine, 丨, and cardiac diazepine. Dian and 1,2,5,6-tetrahydropyridine, and acryl ring; RR, R, R, and R are independently selected from hydrogen, halogen, alkyl, haloalkyl, control group, alkoxy, and fluorene Alkoxy, pentathio, alkylthio, cyano, nitro, alkylcarbonyl, alkoxycarbonyl, aryl or aryloxy, the prerequisites are at least one of R2, R3, R4, and H6 Not hydrogen; and either R2 and R3, or R3 and R4 and -〇CF2〇-, -〇CF2CF2-, -CF2CF2〇, or _CH = CHCH = CH- to form a benzo-fused ring; and in ( a) when m and η are 0; then a double bond is formed between the methyl carbon (a) and the 4-position of the 6-membered acyl ring, 90038 200427680 Where B is phenyl substituted with R9, R1G, R11, R12 and R13, and R9 R12 in which R9, R1G, R11, R12 and R13 are independently selected from hydrogen, halogen, alkyl, haloalkyl, hydroxyl, alkoxy, haloalkoxy, sulfhydryl and alkylthio, cyano, and alkylcarbonyl , Alkoxycarbonyl or aryloxy; and wherein either R9 and R10, or R10 and Ru are taken together with -〇CF2〇-, -〇CF2CF2- or -CF2CF2C)-to form a benzo-fused ring; and When (b) m is 1 and η is 0, then a double bond is formed between the methyl carbon (a) and the 4-position of the 6-membered acryl ring, 90038 200427680 R In 4RR3, β is a bridging group from methyl (a) to r; where B is selected from 0, S, * CH2〇, * 〇CH2, oc (= o) o, * oc (= o) nr15, * NR15C (= 0) 〇, * 〇C (= S) NR15, * NR15C (= S) 0, * 〇ch2c (= 〇) nr15, * nr15c (= 〇) ch2o, * ch2oc (= o) nr15, * NRi5C (= 0) 〇CH2, * NRi5CH2, * ch2nr15, * NR15C (= 〇), * C (= 〇) NR15, * NR15S〇2, * S〇2NR15, * NRi5NHS02, * S02NHNR15, * 0C (= 0 ) NRi5S02, * s〇2nr15c (= o) o, * 〇c (= 〇) nr15chr16, * chr16nr15 c (= 0) 0, * NR15C (= 0) NR16, 1,4-dioxocyclohexyl or 4- Oxyhexahydropyridin-1-yl, where the asterisk represents the point of attachment to methyl carbon (a); where Rb and R16 are independently selected from hydrogen, alkyl, alkylaminocarbonyl, and arylcarbonyl, where aryl is regarded as It needs to be substituted with halo, alkynyl, alkoxy, halofluorenyl, haloalkoxy or nitro; where R is alkyl, cycloalkyl, alkenyl or alkoxycarbonyl; or 90038 200427680 R is R17 , R18, R19, R2G and R21 substituted phenyl; RJ7 r20 or R is a pyridin-2-yl group substituted with R18, R19, R20 and R21, Or Tondo-3-yl substituted with R17, R19, R20 and R21, 90038 -4- 200427680 R19, R2. And R21 is substituted by pyridin-3-yl, 19 of which R17, R18, R19, R20 and R21 are independently selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, etc. | Alkylthio, cyano, nitro, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylamino, aryl, aryloxy, and 2-alkyl-2H-tetrazole, and one of them may be R17 or R18 Or take R18 and can form a benzo-fused ring together with _CH2CH = CHCHr, -ocf2o-, -〇cf2cf2-, or -CF2CF2〇; and (c) m and η are 1; then in 6-membered acryl A single bond is formed between the &amp; base carbon of the ploughing ring and the 4_ position, R4 R · ' Where B is a bridging group from methyl carbon (a) to R; where 90038 200427680 B is selected from 〇, S, * CH2〇, * 〇CH2, 〇C (= 〇) 〇, * 0C (= 0) NR15 * NR15C (= 〇) 〇, * 〇C (= S) NR15, * NR15C (= S) 〇, * 〇CH2C (= 〇) NR15, * NR15C (= 〇) CH20, * CH2〇C (= 〇) ) NR15, * NR15C (two) 〇CH2, * NR15CH2, * CH2HR15, * NR15C (= 〇), * C (= 0) NR15, * NR15S〇2, * S〇2NR15, * NR15NHS〇2, * so2nhnr15 , * 〇c (= 〇) nr15so2, * S02NRl5C (= 0) 0 ^ * 0C (= 0) NRl5CHR16 &gt; * chr16nr15 C (= 〇) 0, * NR15C (= 0) NR16, 1,4-dioxane Cyclohexyl or 4-oxyhexahydroppyridin-1-yl, where the asterisk represents the point of attachment to methyl carbon (a); where R15 and R16 are as described above; and R is an alkyl, cycloalkyl, or olefin Or alkoxycarbonyl; or R is phenyl substituted with R17, R18, R19, R20, and R21; pyridin-2-yl substituted with Ri8, R19, R20, and R21; substituted with R17, R19, R2Q, and R21 Pyridin-3-yl; pyridin-4-yl substituted with R17, R18, R2G, and R21; or pyridin-3-yl substituted with R19, R20, and R21; of which Ri7, R18, R19, R2 0 and R21 are as described above; R is selected from hydrogen, alkynyl, alkynyl, or aryl; when P is 1, 2, or 3; D is -CHr, and forms a 6-membered nitrogen ring Heterobicyclic derivatives; when q is 0 and r is 1, it will form a 6-membered acyclic nitrogen oxide derivative; when q is 1 and r is 0 or 1, 90038 -6- 200427680 R is selected From alkyl, alkyl, hydroxyalkyl, alkoxyalkyl, dialkylaminoalkyl, alkylaminocarbonyloxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, alkylcarbonyl Oxyalkyl, alkoxycarbonylalkyl, carboxyalkyl, + pit, arylcarbonyl, sulfonate or sulfonate alkyl, and can carry negative charges to form internal salts; and separate ionic chlorides, bromine Compounds, iodides, or sulfuric acid or alkyl sulfonates or phenyl esters; when s is 0 or 1; R is selected from the group consisting of hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkoxy, and alkoxy: radical, amino, morphinyl, optionally substituted indolyl, hexahydropyridyl, Optionally substituted (pyridyl) alkenyl, optionally substituted 1,2,3,4-tetrahydrofluorenyl, optionally substituted arylpyrazolyl, benzo [b] thienyl, 5-Hydropyrido n, 2a] pyrimidinone, 4-Hydroxy-1,3-pyridine fully leached and [3,2a] pyridinone, 1,2,3,4- Tetrahydroquinolinyl, 2-thio- 丨,% dihydroquinazolinone, 1,3-dihydroquinazolinone, or benzo [c] azepinedione, Among them, the essential substituents of S are selected from the group consisting of halide, fluorenyl, alkoxy, and nitro; or R8 is a phenyl substituted with R22, R23, R24, and r26, 90038 or R 23 200427680 pyridin-2-yl substituted with R23, R24, R25 and R26 R 22 23 R r26 / γ \ r24 25 R or pyridin-3-yl substituted with R22, R24, R25 and R26 23, 26 R 24 R 25 or pyridin-4-yl substituted with R22, R23, R25 and R26 R 22 R 24 R wherein R22, R23, R24, R25 and R26 are independently selected from the group consisting of hydrogen, halogen, alkyl, hydroxy, alkoxy, alkoxy, alkoxy, alkoxy, Alkoxyiminoalkyl, alkenoxyiminoalkyl, alkynoxyiminoalkyl, cycloalkylalkoxy, alkoxyalkoxy, alkylthio, dithioalkoxy Alkyl, trithioalkoxyalkyl, alkylsulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, cycloalkyl 90038 amino groups, sS groups, fluorenyloxy, fluorenyloxy, Diluted oxy group, alkoxy group, optionally substituted aryl group, cyano group, nitro group, amine group, alkylamino group, alkylcarbonylamino group, alkoxycarbonylamino group, alkenyloxy group Carbonylamino, alkynyloxycarbonylamino, haloalkylcarbonylamino, alkoxyalkoxycarbonylamino, (alkyl) (alkoxycarbonyl) amino, alkylsulfonylamino, Substituted (heteroaryl) (alkoxycarbonyl) amino group as needed, substituted arylcarbonylamino group as needed, formamyl group, substituted 1,3-dioxolane-2-yl as needed 1, if necessary, replaced by 1,3- Dioxane-2-yl, optionally substituted 1,3-oxazolidin-2-yl, optionally substituted 1,3-oxazaperhydroin-2-yl, optionally substituted 1, 3-dithiacenyl-2-yl, optionally substituted 1,3-dithiazane-2-yl, alkoxycarbonyl, alkylaminocarbonyloxy, alkylaminoalkylamino, dihuo Aminoamino, thioamino (thiothio) amino, dialkylphosphourea, optionally substituted thienyl, optionally substituted 1,3-thiazolylalkoxy, Optionally substituted aryl, optionally substituted aryloxy, optionally substituted aryloxyalkyl, optionally substituted arylaminocarbonyloxy, optionally substituted heteroaryl, optionally Requires substituted heteroaryloxy, optionally substituted pyrrolyl, optionally substituted pyrazolyl, optionally substituted pyridoxy, optionally substituted 1,3-oxazole 4-yl 1, substituted 1,3-oxazolineoxy group if necessary, substituted 1,3-oxazoline amino group as needed, substituted 1,2,4-triazolyl group as needed, Substituted 1,2,3 oxazolyl, as required Substituted 1,2,5-fluoradiazolidyl, optionally substituted 1,2,5-thiadiazolyl 200427680 radical, substituted 2 fluorenyl · tetrazolyl radical if necessary, substituted 17-pyridine if necessary Base, optionally substituted pyridyloxy, optionally substituted pyridylamino, optionally substituted pyrimidinyl, optionally substituted pyrimidinyloxy, optionally substituted 3,4,5,6- Tetrahydropyrimidinyloxy, optionally substituted pyridoxy, or optionally substituted 1,2,3,4-tetrahydrofluorenyl, wherein the optionally substituted group is selected from one or more halogens , Alkynyl, i-alkynyl,:!: Pentyloxy, dialkyloxyalkyl, dithioalkoxyalkyl, cyano, nitro, amino, or alkoxycarbonylamino, the prerequisites are At least one of R22, R23, R24, R25 and R26 is not hydrogen; when s is 1; E is selected from (CR27R28) x- (CR29R30) y, (CR27R2s) HCR29R3〇) y〇 *, C3H6, C4H8, c (= 0), C (= 〇) C2H4 *, c2h4c (= 〇) *, C3H6C (= 0) *, C4H8NHC (= 〇) *, or C (= S) NH * bridge base, where the asterisk represents R8 Followed by where X is 1; y is 0 or 1; and R27, R28, R29 and are independently selected from optionally r3〇 system to replace the heavy atmosphere alkoxy, alkyl and aryl; N-oxide; and its agriculturally acceptable salts. 2. The compound according to item 1 of the scope of patent application, wherein p and q are 0;! · Is 0 90038 -10- 200427680 Or 1; and s is 1; R2, R3, R4, R5, and R6 are independently selected from hydrogen, halogen, pit group, alkyl, hydroxy, alkoxy, i-alkoxy, pentahalothio, and sulfur burning Group, nitro, aryl and aryloxy; E- (CR27R28) x- (CR29R30) y- bridging group (where X is 1 and y are 0, R27 and R28 are hydrogen); and R8 is R22, R23, R24, R25 and R26 substituted phenyl groups, wherein R22, R23, R24, R25 and r26 are independently selected from hydrogen, alkoxy, dialkoxyalkyl, dithioalkoxyalkyl, alkoxy Iminoalkyl, alkenoxyiminoalkyl, alkynoxyiminoalkyl, alkoxycarbonylamino, optionally substituted arylcarbonylamino, alkoxycarbonyl, alkylaminocarbonyl Oxy, optionally substituted 1,3-dioxolane-2-yl, optionally substituted 1,3-dioxane-2-yl, optionally substituted 1,3-dioxolane-2-yl Dithiacenyl-2-yl, optionally substituted 1,3-dioxan-2-yl, optionally substituted aryl, optionally substituted aryloxy, optionally substituted 2H- Tetrazole, optionally substituted pyridyl, optionally substituted p-pyridyloxy, optionally The bite call group, the optionally substituted pyrimidinyloxy, and optionally substituted pyridazin the farming group. 3. The compound according to item 2 of the scope of patent application, wherein A is C and forms the hexahydropyridine ring; m is (a) 0 or (b) l and η is 0, and the methyl carbon (a) and the six A double bond is formed between the 4-positions of the hydrogen outer ring; and (a) m and η are 0; Β is a phenyl substituted with R9, R1G, R11, R12, and R13, of which R9, R10, R11 , R12 and R13 are independently selected from the group consisting of hydrogen, halogen, fluorenyl, halo, light, halooxy, sulfhydryl, and thiothio; or 90038 -11- 200427680 in (b) m system 1 and η Hour 0; B is a bridging group selected from 〇, * 〇C (= 〇) NR15 and * S〇2NR15, where R15 is hydrogen; and R is a phenyl substituted with R17, R19, R20 and r2i, where Ri7, R18, R19, and R2i are independently selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkoxy, nitro, aryl, aryloxy, and 2-:) ¾-2H -Four π sit. 4. The compound according to item 3 of the scope of patent application, wherein R2, R3, R4, rS, and R6 are independently selected from the group consisting of hydrogen, halogen, haloalkyl, and haloalkoxy; and R22, R R, and R. And R26 are independently selected from hydrogen, dialkoxyalkyl, dithioalkoxyalkyl, alkoxyiminoalkyl, alkylaminocarbonyloxy, as needed, &amp; substituted, 3-, Dioxolane-2-yl, optionally substituted 1,3-dioxane-2-yl, optionally substituted aryloxy, optionally substituted Sijun, substituted if necessary Pyridinyloxy, optionally substituted mannanyl, optionally substituted pyrimidinyloxy, and optionally substituted pyridinyloxy. ^ According to item 4 of the scope of patent application, wherein (a) m &amp; n is 0; and R, H10, R11, feet 12 and feet 13 are independently selected from hydrogen, halogen, haloalkyl, and haloalkoxy . The compound according to item 5 of the scope of patent application, wherein R2, R3, R5, R6, R, R10, R12, R13, R22, r23, r25 and r26 are hydrogen; R4 &amp; R11 is difluoromethyl, trifluoromethyl Or trifluoromethoxy; and R24 is pyridin-2-oxy 90038, 12-200427680 or pyrimidin-2-oxy. 1. The compound according to item 4 of the scope of patent application, wherein (b) m is 1 and η is 0; ^ is 0 or * 〇C (= 0) NR15 bridging group; and R17, R18, R19, R20, and R21 are Independently selected from the group consisting of hydrogen, dentin, alkyl, and || alkoxy. 8. The compound according to item 7 of the scope of patent application, wherein R2, R3, R5, R6, R17, R18, R20, R2i, R22, r23, r25 and r26 are hydrogen; r4 &amp; r19 is difluoromethyl, tri Fluoromethyl or trifluoromethoxy; and R24 is pyridin-2-oxy or pyrimidin-2-oxy. 9. The compound according to item 2 of the scope of the patent application, in which eight systems of CH form the hexahydropyridine ring; (c) m and n systems of 1, form a single bond between the methyl carbon and the kernel position of the ring; R1 Is hydrogen; B is a bridging group selected from 〇, * 〇C (= 〇) NR15 and * S〇2NR15, wherein R15 is hydrogen; and R is phenyl substituted with Ri7, Ris, r19, r20 and r21, Where r17, r18, ^, Han and R are independently selected from the group consisting of hydrogen, halogen, halo, halo, alkoxy, haloalkoxy, nitro, aryl, aryloxy, and 2-alkyl-2H -Shiguchi 0 10 · The compound according to item 9 of the scope of the patent application, wherein R2, R3, R4, R5 and R are independently selected from hydrogen, halogen, self-igniting group and drawoxy group; and R22, RR, R25 and r26 are independently selected from the group consisting of hydrogen, dialkoxyalkyl, dithioalkoxyalkyl, alkoxyiminoalkyl, alkylaminocarbonyloxy, and optionally substituted, 3-dioxolane-2-yl, substituted if necessary, 3-dioxo 90038 -13- 200427680 heterocyclohexane-2-yl, substituted aryloxy if necessary, substituted if necessary 2H-tetrazole, optionally substituted pyridyloxy 2. Orally substituted cypher groups as needed, substituted pyrimidinyloxy groups as needed, and healthy oxy groups substituted as needed. 11. 12. 13. 14. 15. 16. 17. The compound according to item 10 of the scope of patent application, wherein β is 〇 or * 〇C (= 〇) NR15 bridging group; R17, Ris, ri9, R2〇 and r21 The system is independently selected from hydrogen, autogen, haloalkyl, and haloalkoxy. The compound according to item 11 of Shenyan's patent scope, in which R2, Han3, Trans5, =, R17, R18, R20 'R21, R22, R23, R25, and R26 are hydrogen; and R19 is difluoromethyl, tri Fluoromethyl or trifluorofluorenyloxy; and KM-based pyridine-2-oxy or oxo-2-oxy. A composition comprising at least one agriculturally acceptable bulking j or admixture &amp; at least one insecticidally effective amount of a compound such as the one described in Patent Park. -A kind of composition "纟 includes at least one kind of agriculturally acceptable increase ^ 丨 丨 J or adjuvant at least one insert, but the dry girl, ^ ^ set insects effective, such as applying for a patent | &gt; The compound of item 2 of the garden. -A composition comprising at least-an insecticidally effective amount of a compound as claimed in claim 3 in combination with at least-agriculturally acceptable alternatives or agents or adjuvants. The seed composition &apos; includes at least one compound of item 4 in combination with at least one agriculturally acceptable additive or adjuvant. A beta patent-a composition comprising an agriculturally acceptable increase of 90038 -14-200427680 18. Dizo: at least one insecticidally effective amount of the compound compounded in the item of the patent application). Seven compositions' which include at least-an insecticidally effective amount of a compound as specified in item 6 above, in combination with at least one agriculturally acceptable increase. 19. 20. 21. 22. 23. A composition which includes at least one kind of heartworm that is effective in admixture with at least one agriculturally acceptable agent or adjuvant as described in the patent application scope 7 Item &lt; Compound. A compound comprising at least one agriculturally acceptable amount of at least one kind of insecticidally effective amount of an insecticidally effective compound such as the eighth meaning compound in the patent claim. A composition &apos; comprising at least one insecticidally effective amount of the compound of item 9 in combination with at least one agriculturally acceptable extender or adjuvant. A composition comprising at least one insecticidally effective amount of a compound as claimed in claim 10 in combination with at least one agriculturally acceptable extender or adjuvant. A composition comprising at least one insecticidally effective amount of a compound as claimed in claim 11 in combination with at least one agriculturally acceptable extender or adjuvant. 24. 25. A composition comprising at least one insecticidally effective amount of a compound as claimed in item 12 of the patent application, in combination with at least one agriculturally acceptable extender or adjuvant. The insecticidal composition according to item 13 of the Chinese Patent Application, which still includes the first 90038 -15-200427680 or a plurality of second-type compounds. 26. The insecticidal composition according to item 14 of the application, which further comprises one or more compounds of the second type. 27. The insecticidal composition according to item 15 of the scope of patent application, which further comprises one or more compounds of the second type. 28. The insecticidal composition according to item 16 of the application, which further comprises one or more compounds of the second type. 29. An insecticidal composition according to item 17 of the scope of patent application, which further comprises one or more compounds of the second type. 3 (λ The insecticidal composition according to item 18 of the patent application, which further comprises one or more compounds of the second type. 31. The insecticidal composition according to item 19 of the patent application, which further comprises one or more second compounds 32. The insecticidal composition according to claim 20 of the application, which further comprises one or more compounds of the second type. 33. The insecticidal composition according to claim 21 of the application, which further comprises one or more Second class of compounds. 34. The insecticidal composition according to item 22 of the patent application, which further comprises one or more second class of compounds. 35. The insecticidal composition according to item 23 of the patent application, which further comprises a Or multiple second class compounds. 36. The insecticidal composition according to item 24 of the application, which further comprises one or more second class compounds. 37. A method for controlling insects, comprising an insecticidally effective amount of For example, application 90038 -16- 200427680 38. 39. 40. The composition of the scope of patent No. 13 is sprayed on the place where there is or is expected to be insects. A method for controlling insects, comprising An insecticidally effective amount of the composition as described in item 14 of the patent application scope is sprayed on the place where there is or is expected to be insects ^ A method for controlling insects, which comprises an insecticidally effective amount of the combination as described in item 15 of the patent application range A substance is sprayed on a place where there is or is expected to be insects. A method for controlling insects, which comprises spraying a composition with an insecticidally effective amount such as the item in the scope of patent application No. 16 on the presence or expectation of insects :: 41.-A method for controlling insects, comprising applying an insecticidally effective amount of a composition as claimed in item 17 of the patent application in the presence or expected presence of insects :: a site. 42. 43.-A method for controlling insects A method comprising applying an insecticidally effective amount of a composition such as in the scope of patent application No. 18 to a place where insects are present or expected:-A method of controlling insects comprising an insecticidally effective amount such as 44. 45. A method of controlling insects, which includes an insecticidally effective amount of a combination as described in claim 20 Shi Li is in a place where there is or is expected to be insects.-A method for controlling insects, which includes an insecticidally effective amount such as application 90038 -17- 200427680 46. 47. 48. 49. 50. 51. 52. 53. The composition of the scope of the patent No. 21 is applied to the place where there is or is expected to be insects. A method of controlling insects, which comprises applying the composition of the scope of the No. 22 of the patent scope of Shenjing with an insecticidally effective amount. Wei is in a place where there is or is expected to be an insect. A method of controlling insects, which includes an insecticidally effective amount of a composition such as Shi Li in the scope of the patent application No. 23, where Shi Li is present or is expected to have a place. A method for controlling insects, comprising applying an insecticidally effective amount of a composition such as in the scope of application No. 24 to a place where insects are present or expected to be present. A method for controlling insects, which comprises applying an insecticidally effective amount of a composition such as in the scope of application No. 25 to a place where insects are present or expected to be present. A method for controlling insects, comprising applying an insecticidally effective amount of a composition such as in the scope of application No. 26 to a place where insects are present or expected to be present. A method for controlling insects', comprising applying an insecticidally effective amount of a composition such as in the scope of application No. 27 to a place where insects are or are expected to be present. A method for controlling insects, which comprises applying an insecticidally effective amount of a composition such as in the scope of application No. 28 to a place where insects are present or expected to be present. A method for controlling insects, which comprises an insecticidally effective amount of a composition such as the application 90038 -18- 200427680 54. 55. 56. 57. 58. 59. 60. The scope of the patent "in the presence or prospect of insects Existing place. A method for controlling insects, which contains insecticidally effective #_ If the composition of the patent scope item 3G is applied to the place where there is or is expected to be insects: a place.-A method for controlling insects, which The composition containing an insecticidally effective amount such as the scope of the patent application item 31 is in the place where there is or is expected to be insects. A method for controlling insects, which includes an insecticidally effective amount of the Ruoshen patent range No. The composition of item 32 is sprayed on a place where there is or is expected to be insects. 2. A method for controlling insects, comprising applying an insecticidally effective amount of the composition such as the item 33 of the patent application to or is expected to have insects Existing place. A method for controlling insects, comprising applying an insecticidally effective amount of a composition such as in the scope of patent application No. 34 to a place where there is or is expected to be insects. An insect-preparing method comprising applying an insecticidally effective amount of a composition such as item 35 of the patent application scope to or in the presence of insects = a place. An insect-controlling method comprising an insecticidally effective amount If the composition in the scope of application for patent No. 36 is applied to the place where there is or is expected to be insects = 90038 -19-200427680 柒, the designated representative map: (I) The designated representative map in this case is: (none) (two) A brief description of the element representative symbols in this representative figure: 捌 If there is a chemical formula in this case, please disclose the chemical formula that best shows the characteristics of the invention: I 90038